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CDKI-73

Catalog No. T14919   CAS 1421693-22-2

CDKI-73 is a potent CDK9 inhibitor (Ki: 4 nM). It shows selective toxicity to CLL cells(LD50=80 nM) versus normal B cell and normal CD34+ cell(LD50<20 uM).The inhibition of CDK9 induces apoptosis and potentiates the effect of cisplatin.

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CDKI-73 Chemical Structure
CDKI-73, CAS 1421693-22-2
Pack Size Availability Price/USD Quantity
1 mg In stock $ 146.00
2 mg In stock $ 198.00
5 mg In stock $ 308.00
10 mg In stock $ 443.00
25 mg In stock $ 732.00
50 mg In stock $ 987.00
100 mg In stock $ 1,390.00
1 mL * 10 mM (in DMSO) In stock $ 323.00
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Purity: 98.11%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description CDKI-73 is a potent CDK9 inhibitor (Ki: 4 nM). It shows selective toxicity to CLL cells(LD50=80 nM) versus normal B cell and normal CD34+ cell(LD50>20 uM).The inhibition of CDK9 induces apoptosis and potentiates the effect of cisplatin.
Targets&IC50 CDK6:37.68 nM, CDK2:3.27 nM, CDK9:5.78 nM, CDK4:8.18 nM, CDK7:134.26 nM, CDK1:8.17 nM
In vitro CDKI-73, one of the most potent CDK9 inhibitors, against a panel of AML cell lines and samples derived from 97 patients.?CDKI-73 induced cancer cells undergoing apoptosis through transcriptional downregulation of anti-apoptotic proteins Bcl-2, Mcl-1 and XIAP by majorly targeting CDK9[3].
In vivo CDKI-73 exhibited a favorable pharmacokinetic profile with oral bioavailability of F = 56% following a single intravenous bolus dose at 2 mg/kg and an oral dose at 10 mg/kg in mice [1].
Molecular Weight 394.45
Formula C15H15FN6O2S2
CAS No. 1421693-22-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 52 mg/mL (131.83 mM)

TargetMolReferences and Literature

1. Xie S, et al. Antitumor action of CDK inhibitor LS-007 as a single agent and in combination with ABT-199 against human acute leukemia cells. Acta Pharmacol Sin. 2016 Nov;37(11):1481-1489. 2. Lam F, et al. Targeting RNA transcription and translation in ovarian cancer cells with pharmacological inhibitor CDKI-73. Oncotarget. 2014 Sep 15;5(17):7691-704. 3. CDKI-73: an orally bioavailable and highly efficacious CDK9 inhibitor against acute myeloid leukemia.[J]. Investigational new drugs, 2018.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Anti-Cancer Compound Library Bioactive Compounds Library Max Kinase Inhibitor Library NO PAINS Compound Library Anti-Pancreatic Cancer Compound Library Orally Active Compound Library Anti-Breast Cancer Compound Library Inhibitor Library Anti-Aging Compound Library

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Keywords

CDKI-73 1421693-22-2 Apoptosis Cell Cycle/Checkpoint CDK toxicity Inhibitor low AML Acute LS 007 myeloid LS007 leukemia CLL LS-007 endosome Cyclin dependent kinase CDKI 73 CDKI73 inhibit inhibitor

 

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