Home Angiogenesis Bcr-Abl inhibitor Bafetinib For research use only.

Bafetinib

Synonyms: INNO-406, NS-187

Bafetinib is a potent and selective dual Bcr-Abl/Lyn inhibitor with IC50 of 5.8 nM/19 nM in cell-free assays, does not inhibit the phosphorylation of the T315I mutant and is less potent to PDGFR and c-Kit.

Bafetinib Chemical Structure

Bafetinib Chemical Structure

CAS No. 859212-16-1

Purity & Quality Control

Bafetinib Related Products

Signaling Pathway

Bcr-Abl Signaling Pathways

Bcr-Abl Signaling Pathway

Biological Activity

Description Bafetinib is a potent and selective dual Bcr-Abl/Lyn inhibitor with IC50 of 5.8 nM/19 nM in cell-free assays, does not inhibit the phosphorylation of the T315I mutant and is less potent to PDGFR and c-Kit.
Features Dual Bcr-Abl/Lyn inhibitor.
Targets
Abl [1]
(Cell-free assay)		 Lyn [1]
(Cell-free assay)
5.8 nM 19 nM
In vitro
In vitro

Bafetinib blocks WT Bcr-Abl autophosphorylation and its downstream kinase activity with IC50 of 11 nM and 22 nM in K562 and 293T cells, respectively. Bafetinib suppresses the growth of the Bcr-Abl-positive cell lines including K562, KU812, and BaF3/wt cells potently without effects on the proliferation of the Bcr-Abl-negative U937 cell line. Moreover, Bafetinib exhibits a dose-dependent antiproliferative effect against Bcr-Abl point mutant cell lines, such as BaF3/E255K cells. [1] In Bcr-Abl+ leukemia cell lines, Bafetinib induces both caspase-mediated and caspase-independent cell death by blocking the phosphorylation of Bcr-Abl. [2]
Kinase Assay Kinase assay
Bcr-Abl kinase assays are performed in 25 μL of reaction mixture containing 250 μM peptide substrate, 740 Bq/μL [γ-33P]ATP, and 20 μM cold adenosine triphosphate (ATP) by using the SignaTECT protein tyrosine kinase assay system. Each Bcr-Abl kinase is used at a concentration of 10 nM. Kinase assays for Abl, Src, and Lyn are carried out with an enzyme-linked immunosorbent assay (ELISA) kit. The inhibitory effects of NS-187 against 79 tyrosine kinases are tested with KinaseProfiler.
Cell Research Cell lines K562, BaF3/wt, BaF3/E255K, and BaF3/T315I cells
Concentrations 0-10 μM
Incubation Time 72 hours
Method

K562, BaF3/wt, BaF3/E255K, and BaF3/T315I cells are plated at 1 × 103 in 96-well plates, whereas KU812 and U937 cells are plated at 5 × 103 in 96-well plates. Cells are incubated with serial dilutions of Bafetinib for 3 days. Cell proliferation is measured by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide; Nacalai Tesque) assay, and the 50% inhibitory concentration (IC50) values are calculated by fitting the data to a logistic curve.
In Vivo
In vivo

In Bcr-Abl–positive KU812 mouse model, Bafetinib (0.2 mg/kg/day) significantly inhibits tumor growth, and completely inhibits tumor growth without adverse effects at 20 mg/kg/day. For Balb/c mice, Bafetinib shows maximal tolerated dose of 200 mg/kg/d and bioavailability value (BA) of 32%. [1] In a Central nervous system (CNS) leukemia model bearing Ba/F3/wt bcr-ablGFP, Ba/F3/Q252H, or Ba/F3/M351T cells, combination treatment of Bafetinib (60 mg/kg) and CsA (50 mg/kg) leads to more significant inhibition of leukemia growth in the brain than either Bafetinib or CsA alone. [3]
Animal Research Animal Models KU812 xenograft is established by subcutaneous injection of KU812 cells into the right flank of Balb/c-nu/nu female mice.
Dosages ≤20 mg/kg/day
Administration Administered via p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00352677 Completed
Chronic Myeloid Leukemia|Acute Lymphocytic Leukemia
CytRx
 July 2006 Phase 1

Chemical Information & Solubility

Molecular Weight 576.62 Formula

C30H31F3N8O
CAS No. 859212-16-1 SDF Download Bafetinib SDF Download Bafetinib SDF
Smiles CC1=C(C=C(C=C1)NC(=O)C2=CC(=C(C=C2)CN3CCC(C3)N(C)C)C(F)(F)F)NC4=NC=CC(=N4)C5=CN=CN=C5
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (173.42 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

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.

Handling Instructions

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Frequently Asked Questions

Question 1:
Can you suggest the route of in vivo administration for S1369?

Answer:
S1369 in 0.5% methylcellulose+0.2% Tween 80 at 30mg/ml is a suspension, and it is fine for oral gavage. If you dissolved the compound in 0.5% methyl cellulose and got a suspension, it is fine. And 0.2% Tween 80 can help the suspension dissolving more homogeneous.

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