Home Cell Cycle CDK inhibitor CDKI-73 For research use only.

CDKI-73

CDKI-73 (LS-007) is a potent CDK inhibitor in vitro with IC50 of 8.17 nM, 3.27 nM, 8.18 nM, and 5.78 nM for CDK1, CDK2, CDK4, and CDK9, respectively. CDKI-73 induces apoptosis in cancer cells. CDKI-73 is an orally bioavailable and highly efficacious CDK9 inhibitor against acute myeloid leukemia.

CDKI-73 Chemical Structure

CDKI-73 Chemical Structure

CAS No. 1421693-22-2

Purity & Quality Control

CDKI-73 Related Products

Signaling Pathway

CDK Signaling Pathways

CDK Signaling Pathway

Biological Activity

Description CDKI-73 (LS-007) is a potent CDK inhibitor in vitro with IC50 of 8.17 nM, 3.27 nM, 8.18 nM, and 5.78 nM for CDK1, CDK2, CDK4, and CDK9, respectively. CDKI-73 induces apoptosis in cancer cells. CDKI-73 is an orally bioavailable and highly efficacious CDK9 inhibitor against acute myeloid leukemia.
Targets
CDK2 [1]
(Cell-free assay)		 CDK9 [1]
(Cell-free assay)		 CDK1 [1]
(Cell-free assay)		 CDK4 [1]
(Cell-free assay)
3.27 nM 5.78 nM 8.17 nM 8.18 nM
In vitro
In vitro

CDKI-73 induces cancer cells undergoing apoptosis through transcriptional downregulation of anti-apoptotic proteins Bcl-2, Mcl-1 and XIAP by majorly targeting CDK9. Contrastively, it is relatively low toxic to the bone marrow cells of healthy donors.[2]
Cell Research Cell lines Leukemia cell lines (MOLM13, MV4-11, THP-1, etc.)
Concentrations 0.05 μM, 0.1 μM, 0.25 μM, 0.5 μM
Incubation Time 1 h, 4 h, 12 h, 24 h, 48 h
Method

MV4-11 (1 × 105/well) cells are seeded and incubated under 5% CO2 at 37ºC overnight. After incubation with indicated concentrations of the CDKI-73 for 24 or 48 h, cells are collected and centrifuged (300 g, 5 min). For cell cycle assay, the pellets are re-suspended in cold 70% ethanol and fixed on ice for 15 min, followed by centrifugation (300 g, 5 min). The collected pellets are incubated with 200 μL staining solution at 37ºC for 1 h, then analyzed with a Gallios flow cytometer. Apoptosis is assessed with cells collected and processed as per the instruction in the annexin V-FITC/PI commercial kit.
In Vivo
In vivo

CDKI-73 is orally bioavailable, highly efficacious against MLL-AML MV4–11 xenografts and downregulates anti-apoptotic proteins by targeting CDK9 in vivo.[2]
Animal Research Animal Models female nude (nu/nu) Balb/C mice aged 6–8 weeks
Dosages 25 mg/kg
Administration Oral gavage

Chemical Information & Solubility

Molecular Weight 394.45 Formula

C15H15FN6O2S2
CAS No. 1421693-22-2 SDF --
Smiles CC1=C(SC(=N1)NC)C2=NC(=NC=C2F)NC3=CC(=CC=C3)S(=O)(=O)N
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 79 mg/mL ( (200.27 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 1.5 mg/mL

Water : Insoluble


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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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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