Home Metabolism Casein Kinase inhibitor - Autophagy activator - Apoptosis related activator Silmitasertib (CX-4945) For research use only.

Silmitasertib (CX-4945)

Silmitasertib (CX-4945) is a potent and selective inhibitor of CK2 (casein kinase 2) with IC50 of 1 nM in a cell-free assay, less potent to Flt3, Pim1 and CDK1 (inactive in cell-based assay). Silmitasertib induces autophagy and promotes apoptosis. Phase 1/2.

Silmitasertib (CX-4945) Chemical Structure

Silmitasertib (CX-4945) Chemical Structure

CAS No. 1009820-21-6

Purity & Quality Control

Silmitasertib (CX-4945) Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
UM-SCC-1 Clonogenic Assay 0.5-5 μM 14 d DMSO  inhibits clonogenic survival and sphere formation 25379016
U87-MG Growth Inhibition Assay 1/5/10 μM 24/48/72 h DMSO inhibits cell growth both concentration and time dependently 25241897
MDA-MB-231 Function Assay 2/5/10 μM 4 h inhibits serine 529 phosphorylation and the expression of IL-6, IL-8 25153725
MDA-MB-231 Function Assay 2/5/10 μM 4 h decreases the constitutive phosphorylation of both p-S529-p65 and p-S129-Akt 25153725
HCT116  Apoptosis Assay 10 μM 24/48 h DMSO induces apoptosis 24686080
HCT116  Function Assay 10 μM 4 h DMSO causes ER-stress response over the p-eIF2α branch, but does not induce CHOP  24686080
ARPE-19 Function Assay 10 μM 4 h DMSO causes ER-stress response over the p-eIF2α branch, but does not induce CHOP  24686080
HCT116  Growth Inhibition Assay 10 μM 24-96 h DMSO inhibits cell growth time dependently 24686080
ARPE-19 Growth Inhibition Assay 10 μM 24-96 h DMSO inhibits cell growth time dependently 24686080
ARPE-19 Kinase Assay 5/10/20 μM 24/48 h inhibits CK2 kinase activity at a concentration of 5 μM 24686080
SUP-B15 Apoptosis Assay 6/10 μM 48 h induces apoptosis 24561792
Nalm6  Apoptosis Assay 6/10 μM 48 h induces apoptosis 24561792
SUP-B15 Function Assay 10/20 μM 24 h results in decreased PTEN phosphorylation at the CK2 target residue S380 and concomitant downregulation of PTEN protein expression 24561792
Nalm6  Function Assay 10/20 μM 24 h results in decreased PTEN phosphorylation at the CK2 target residue S380 and concomitant downregulation of PTEN protein expression 24561792
C2C12 Function Assay 3 μM 12/24/48 h inhibits the expression of osteoclast differentiation markers and Akt phosphorylation 24293011
MOLT-4 Apoptosis Assay 5 μM 24/48 h induces apoptosis 24253024
DND-41 Apoptosis Assay 5 μM 24/48 h induces apoptosis 24253024
ALL-SIL Apoptosis Assay 5 μM 24/48 h induces apoptosis 24253024
DND-41 Growth Inhibition Assay 1-10 μM 48 h IC50=9 μM 24253024
HPB-ALL Growth Inhibition Assay 1-10 μM 48 h IC50=6.1 μM 24253024
ALL-SIL Growth Inhibition Assay 1-10 μM 48 h IC50=5.7 μM 24253024
PF-382 Growth Inhibition Assay 1-10 μM 48 h IC50=4.5 μM 24253024
MOLT-4 Growth Inhibition Assay 1-10 μM 48 h IC50=5.7 μM 24253024
CEM-S Growth Inhibition Assay 1-10 μM 48 h IC50=4.6 μM 24253024
CEM-R Growth Inhibition Assay 1-10 μM 48 h IC50=4 μM 24253024
Jurkat Growth Inhibition Assay 1-10 μM 48 h IC50=4.9 μM 24253024
Rec-1 Growth Inhibition Assay 0-40 μM 48 h IC50=1.46 µM  24086494
Jeko-1 Growth Inhibition Assay 0-40 μM 48 h IC50=2.4 µM  24086494
INA-6 Growth Inhibition Assay 0-40 μM 48 h IC50=2.42 µM 24086494
U-266 Growth Inhibition Assay 0-40 μM 48 h IC50=19.8 µM  24086494
A549 Function Assay 3 μM 48 h inhibits TGF-β1-induced activation of Smad and expression of Snail and Twist 24023938
A549 Function Assay 10 μM 12/24/48 h inhibits TGF-β1-induced migration and invasion 24023938
R-LAMA84 Growth Inhibition Assay 2.5-10 μM 48 h DMSO inhibits cell growth concentration dependently 24012109
S-LAMA84 Growth Inhibition Assay 2.5-10 μM 48 h DMSO inhibits cell growth concentration dependently 24012109
R-LAMA84 Function Assay 3 μM 24 h DMSO reduces CK2 activity 24012109
S-LAMA84 Function Assay 3 μM 24 h DMSO reduces CK2 activity 24012109
A549 Function Assay 1/10 μM 48 h DMSO leads to a dose-dependent decrease in Notch reporter activity 23651443
H1299 Growth Inhibition Assay 0-30 μM 72 h DMSO IC50=1.80 μM, inhibits cell growth concentration dependently 23651443
A549 Growth Inhibition Assay 0-30 μM 72 h DMSO IC50=4.15 μM, inhibits cell growth concentration dependently 23651443
LNCap Growth Inhibition Assay 0-30 μM 4 d IC50=4.59 μM 22832316
H2170  Function Assay 10 μM 4-24 h enhances apoptosis with 22387988
A431  Function Assay 10 μM 4-24 h enhances apoptosis with 22387988
H2170  Function Assay 10 μM 30 min attenuates PI3K-Akt-mTOR signaling 22387988
A431  Function Assay 10 μM 30 min attenuates PI3K-Akt-mTOR signaling 22387988
UM-SCC-46 Clonogenic Assay 0.5-5 μM 14 d DMSO  inhibits clonogenic survival and sphere formation 25379016
H28 Growth Inhibition Assay 0.01-30 μM 72 h DMSO IC50=7.2 μM 25422081
H2052 Growth Inhibition Assay 0.01-30 μM 72 h DMSO IC50=2.0 μM 25422081
PC9/GR Function Assay 5 µM 48 h induces autophagy 25486409
PC9/ER Function Assay 5 µM 48 h induces autophagy 25486409
H1299 Growth Inhibition Assay 1/5/10 μM 72 h inhibits cell growth concentration dependently 25750308
Calu-1  Growth Inhibition Assay 1/5/10 μM 72 h inhibits cell growth concentration dependently 25750308
H358 Growth Inhibition Assay 1/5/10 μM 72 h inhibits cell growth concentration dependently 25750308
H1299 Apoptosis Assay 10 μM 72 h induces apoptosis 25750308
Calu-1  Apoptosis Assay 10 μM 72 h induces apoptosis 25750308
H358 Apoptosis Assay 10 μM 72 h induces apoptosis 25750308
NU-DUL Growth Inhibition Assay 5-25 μM 48 h inhibits cell growth concentration dependently 25788269
Oci Ly 3 Growth Inhibition Assay 5-25 μM 48 h inhibits cell growth concentration dependently 25788269
Oci Ly 10 Growth Inhibition Assay 5-25 μM 48 h inhibits cell growth concentration dependently 25788269
Oci Ly 1 Growth Inhibition Assay 5-25 μM 48 h inhibits cell growth concentration dependently 25788269
Oci Ly 18 Growth Inhibition Assay 5-25 μM 48 h inhibits cell growth concentration dependently 25788269
Oci Ly 19  Growth Inhibition Assay 5-25 μM 48 h inhibits cell growth concentration dependently 25788269
Raji Growth Inhibition Assay 5-25 μM 48 h inhibits cell growth concentration dependently 25788269
UM-SCC1 Growth Inhibition Assay 0.1-30 μM 1-5 d IC50=4.1 μM 25798061
UM-SCC46 Growth Inhibition Assay 0.1-30 μM 1-5 d IC50=3.4 μM 25798061
UM-SCC1 Function Assay 0.5/4/10 μM 72 h down-regulates the expression of NF-ĸB, Bcl-XL and up-regulates the expression of p53, p21, AP-1 and IL-8 concentration dependently 25798061
UM-SCC46 Function Assay 0.5/4/10 μM 72 h down-regulates the expression of NF-ĸB, Bcl-XL, p53, p21, AP-1 and up-regulates the expression IL-8 concentration dependently 25798061
HEK293 Kinase Assay 0.5 μM 15 min DMSO reduces CK2 kinase activity 25887626
Hela Kinase Assay 0.5 μM 15 min DMSO reduces CK2 kinase activity 25887626
LAMA84 Kinase Assay 0.5 μM 15 min DMSO reduces CK2 kinase activity 25887626
HEK293 Function Assay 3 μM 5 h DMSO CK2 phosphorylates eIF3j at Ser127 25887626
HDMEC Kinase Assay 1-50 μM 5 h DMSO decreases CK2 kinase activity without affecting cell viability 26189586
HDMEC Function Assay 50 μM 1/5 h DMSO decreases the nuclear signal of phosphorylated p65 in TNF-α-stimulated HDMEC  26189586
A549  Function Assay 3/10 μM 48 h suppresses the micropillar-induced expression of p-FAK 26318800
platelets Kinase Assay 1/5/10 μM 0.5 h DMSO reduces CK2 kinase activity and platelet aggregation 26381437
HDMEC Kinase Assay 0.25/0.5/1 μM 24 h DMSO reduces CK2 kinase activity, vWF expression and secretion 26381437
HDMEC Function Assay 0.25/0.5/1 μM 24 h DMSO reduces expression of VCAM-1 but not ICAM-1 26381437
HDMEC Function Assay 1 μM 24 h DMSO affects subcellular localization of NFATc1 and phospho-p65 26381437
Jurkat Function assay Inhibition of CK2 in human Jurkat cells assessed as inhibition of [gamma33P]ATP incorporation into substrate by luminescence assay, IC50 = 0.1 μM. 21174434
MIAPaCa2 Antiproliferative assay 4 days Antiproliferative activity against human MIAPaCa2 cells after 4 days by alamar blue assay, IC50 = 1.1 μM. 21174434
PC3 Antiproliferative assay 4 days Antiproliferative activity against human PC3 cells after 4 days by alamar blue assay, IC50 = 2.1 μM. 21174434
HCT116 Antiproliferative assay 4 days Antiproliferative activity against human HCT116 cells after 4 days by alamar blue assay, IC50 = 2.2 μM. 21174434
H1299 Antiproliferative assay 4 days Antiproliferative activity against human H1299 cells after 4 days by alamar blue assay, IC50 = 2.4 μM. 21174434
Jurkat Antiproliferative assay 4 days Antiproliferative activity against human Jurkat cells after 4 days by alamar blue assay, IC50 = 2.5 μM. 21174434
A549 Antiproliferative assay 4 days Antiproliferative activity against human A549 cells after 4 days by alamar blue assay, IC50 = 3 μM. 21174434
A375 Antiproliferative assay 4 days Antiproliferative activity against human A375 cells after 4 days by alamar blue assay, IC50 = 3.9 μM. 21174434
BxPC3 Antiproliferative assay 4 days Antiproliferative activity against human BxPC3 cells after 4 days by alamar blue assay, IC50 = 4.4 μM. 21174434
LNCAP Antiproliferative assay 4 days Antiproliferative activity against human LNCAP cells after 4 days by alamar blue assay, IC50 = 4.7 μM. 21174434
K562 Antiproliferative assay 4 days Antiproliferative activity against human K562 cells after 4 days by alamar blue assay, IC50 = 5.3 μM. 21174434
MDA-MB-231 Antiproliferative assay 4 days Antiproliferative activity against human MDA-MB-231 cells after 4 days by alamar blue assay, IC50 = 6.4 μM. 21174434
MCF7 Antiproliferative assay 4 days Antiproliferative activity against human MCF7 cells after 4 days by alamar blue assay, IC50 = 8.9 μM. 21174434
Hs 578T Antiproliferative assay 4 days Antiproliferative activity against human Hs 578T cells after 4 days by alamar blue assay, IC50 = 13.1 μM. 21174434
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells after 72 hrs by MTS assay, IC50 = 5.2 μM. 22339433
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells after 72 hrs by MTS assay, IC50 = 6.5 μM. 22339433
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells after 72 hrs by MTS assay, IC50 = 8.2 μM. 22339433
MV4-11 Antiproliferative assay 1 to 3 days Antiproliferative activity against human MV4-11 cells after 1 to 3 days by MTS assay, CC50 = 3 μM. 23711832
U937 Antiproliferative assay 1 to 3 days Antiproliferative activity against human U937 cells after 1 to 3 days by MTS assay, CC50 = 4.2 μM. 23711832
Jurkat Antiproliferative assay 1 to 3 days Antiproliferative activity against human Jurkat cells after 1 to 3 days by MTS assay, CC50 = 4.5 μM. 23711832
K562 Antiproliferative assay 1 to 3 days Antiproliferative activity against human K562 cells after 1 to 3 days by MTS assay, CC50 = 7 μM. 23711832
Sf9 Function assay Inhibition of CDK2/cyclin E (unknown origin) expressed in Sf9 cells using histone H1 as substrate in presence of [gamma33P]ATP, IC50 = 1.8 μM. 24681986
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells after 72 hrs by MTS assay, CC50 = 9.9 μM. 26850376
Sf21 Function assay 90 mins Inhibition of recombinant human full length N-terminal His6-tagged CK2alpha expressed in Sf21 insect cells using CK2tide as substrate treated for 20 mins measured after 90 mins in presence of MgCl2 by caliper mobility shift assay, IC50 = 0.003 μM. 29559278
Vero E6 Antiviral assay 48 h IC50 for antiviral activity against SARS-CoV-2 in the Vero E6 cell line at 48 h by immunofluorescence-based assay (detecting the viral NP protein in the nucleus of the Vero E6 cells)., IC50 = 3.89045 μM. 32353859
A549 Function assay 30 uM 48 hrs Inhibition of CK2-mediated MMP2 activation in human A549 cells at 30 uM after 48 hrs by gelatin-zymography 24012124
A549 Function assay 10 uM 15 to 30 mins Inhibition of CK2-mediated ERK phosphorylation in human A549 cells at 10 uM after 15 to 30 mins by Western blot method 24012124
A549 Function assay 1 to 10 uM 24 hrs Inhibition of CK2-mediated MT1-MMP expression in human A549 cells at 1 to 10 uM after 24 hrs by Western blot method 24012124
A549 Function assay 10 uM Inhibition of CK2-mediated ERK phosphorylation in human A549 cells at 10 uM by Western blot method 24012124
A549 Function assay 10 uM 24 hrs Inhibition of CK2-mediated AKT phosphorylation in human A549 cells at 10 uM after 24 hrs by Western blot method 24012124
A549 Function assay 10 uM 4 to 24 hrs Inhibition of CK2-mediated AKT phosphorylation in human A549 cells at 10 uM after 4 to 24 hrs by Western blot method 24012124
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
Click to View More Cell Line Experimental Data

Biological Activity

Description Silmitasertib (CX-4945) is a potent and selective inhibitor of CK2 (casein kinase 2) with IC50 of 1 nM in a cell-free assay, less potent to Flt3, Pim1 and CDK1 (inactive in cell-based assay). Silmitasertib induces autophagy and promotes apoptosis. Phase 1/2.
Features First clinical inhibitor of CK2.
Targets
CK2 [1]
(Cell-free assay)
1 nM
In vitro
In vitro

CX-4945 is selective for CK2, as it only inhibits 7 of the 238 kinases by more than 90% at concentration of 0.5 μM, which is 500-fold greater than the IC50 of CK2. Although in cell-free systems CX-4945 inhibits FLT3, PIM1, and CDK1 with IC50 of 35 nM, 46 nM, and 56 nM, respectively, CX-4945 treatment at 10 μM is inactive against FLT3, PIM1, and CDK1 in cell-based functional assays. CX-4945 exhibits a broad spectrum of antiproliferative activity, and the breast cancer cell lines displays the widest range of sensitivity to CX-4945 with EC50 of 1.71-20.01 μM. The antiproliferative activity of CX-4945 correlates with CK2α mRNA and protein levels but not the CK2α' catalytic subunit, the regulatory CK2β subunit, and the PI3K/Akt or PTEN mutational status. CX-4945 inhibits PI3K/Akt signaling by directly blocking the phosphorylation of Akt at Serine 129 by CK2 rather than through activation of PTEN. CX-4945 treatment causes reduced phosphorylation of p21 (T145), increased levels of total p21 and p27, and induction of caspase 3/7 activity. CX-4945 treatment induces a G2/M cell-cycle arrest in BT-474 cells and a G1 arrest in BxPC-3 cells. CX-4945 inhibits HUVEC proliferation, migration, and tube formation with IC50 of 5.5 μM, 2 μM, and 4 μM, respectively. Under hypoxic conditions in BT-474 and BxPC-3 cells, CX-4945 treatment prevents downregulation of p53 and pVHL and reduces activation of HIF-1α transcription. [1] CX-4945 potently inhibits endogenous intracellular CK2 activity with IC50 of 0.1 μM in Jurkat cells. [2]
Kinase Assay CK2 Kinase Assay
CX-4945 is added at a volume of 10 μL to a reaction mixture comprising 10 μL of assay dilution buffer (ADB; 20 mM MOPS, pH 7.2, 25 mM β-glycerolphosphate, 5 mM EGTA, 1 mM sodium orthovanadate, and 1 mM dithiothreitol), 10 μL of substrate peptide (RRRDDDSDDD, dissolved in ADB at a concentration of 1 mM), 10 μL of recombinant human CK2 (ααββ-holoenzyme, 25 ng dissolved in ADB). Reactions are initiated by the addition of 10 μL of ATP solution (90% 75 mM MgCl2, 75 μM ATP (final ATP concentration=15 μM) dissolved in ADB; 10% [γ-33P]ATP (stock 1 mCi/100 μL; 3000 Ci/mM and maintained for 10 minutes at 30 °C. The reactions are quenched with 100 μL of 0.75% phosphoric acid and then transferred to and filtered through a phosphocellulose filter plate. After washing each well five times with 0.75% phosphoric acid, the plate is dried under vacuum for 5 minutes and, following the addition of 15 μL of scintillation fluid to each well, the residual radioactivity is measured using a Wallac luminescence counter. The IC50 values are derived from eight concentrations of CX-4945 over a range of 0.0001 μM to 1 μM.
Cell Research Cell lines SKBr3, MDA-MB-453, BT-474, ZR-75-1, MDA-MB-231, MDA-MB-468, T47D, MCF 7, Hs578T, MDA-MB-361, UACC-812, et al.
Concentrations Dissolved in DMSO, final concentrations ~100 μM
Incubation Time 4 days
Method

Cells are seeded at a density of 3,000 cells per well 24 hours prior to treatment, in appropriate media, and then treated with various concentrations of CX-4945. Suspensions cells are seeded and treated on the same day. Following 4 days of incubation, Alamar Blue (20 μL, 10% of volume per well) is added and the cells are further incubated at 37 °C for 4-5 hours. Fluorescence with excitation wavelength at 530-560 nm and emission wavelength at 590 nm is measured.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-S6K1(T389) / S6K1 / p-S6(S235/236) / S6 p-AKT(S129) / p-AKT(T308) / p-AKT(S473) / AKT / p-ERK / ERK / TP53 / p-p21(Th145) / p21 / Bcl-xl p-Smad2 (Cytosol) / Smad2/3 (Cytosol) / Smad2/3 (Nucleus) / Twist / Snail 30683840
Immunofluorescence β-catenin E-cadherin / Vimentin 24023938
Growth inhibition assay Cell viability 30316146
In Vivo
In vivo

Oral administration of CX-4945 at 25 mg/kg or 75 mg/kg twice daily displays potent antitumor activity in the BT-474 model, with TGI of 88% and 97%, respectively, and 2 of 9 animals in each group showing more than 50% reduction in tumor size compared with the initial tumor volume. In the BxPC-3 model, CX-4945 treatment at 75 mg/kg twice daily shows 93% TGI with 3 animals having no evidence of tumor remaining at the end of the treatment period. [1] In PC3 xenograft model, administration of CX-4945 at 25 mg/kg, 50 mg/kg, or 75 mg/kg causes tumor growth inhibition with TGI of 19%, 40%, and 86%, respectively. [2]
Animal Research Animal Models Female immunocompromised mice CrTac:Ncr-Foxn1nu injected with BxPC-3 or BT-474 cells
Dosages 25 or 75 mg/kg
Administration Oral gavage twice daily
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05817708 Completed
COVID-19
Senhwa Biosciences Inc.
 November 7 2022 Phase 1
NCT04668209 Terminated
Coronavirus
University of Arizona|Senhwa Biosciences Inc.
 January 21 2021 Phase 2
NCT04663737 Completed
Covid19
Chris Recknor MD|Senhwa Biosciences Inc.
 December 3 2020 Phase 2
NCT03904862 Suspended
Medulloblastoma Childhood
Pediatric Brain Tumor Consortium|National Cancer Institute (NCI)|American Lebanese Syrian Associated Charities (ALSAC)
 July 25 2019 Phase 1|Phase 2
NCT02128282 Completed
Cholangiocarcinoma
Senhwa Biosciences Inc.
 June 2014 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 349.77 Formula

C19H12ClN3O2
CAS No. 1009820-21-6 SDF Download Silmitasertib (CX-4945) SDF
Smiles C1=CC(=CC(=C1)Cl)NC2=NC3=C(C=CC(=C3)C(=O)O)C4=C2C=CN=C4
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 70 mg/mL ( (200.13 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Frequently Asked Questions

Question 1:
How to reconstitute the compound (S2248) for in vivo uses?

Answer:
For injection, CX-4945 can be dissolved in 2% DMSO+30% PEG 300+2% Tween 80+ddH2O at 5mg/ml clearly. When making the solution, please dissolve the compound in DMSO clearly first. If it dissolves not readily, please sonicate and warm the solution in water bath at about 45-50℃. Then add PEG and Tween. After they mixed well, dilute with water. For oral gavage, CX-4945 can be dissolved in 1% CMC Na at 30mg/ml as a homogeneous suspension. This is a common formulation for oral gavage, and is convenience to prepare.

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