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CDKI-73

Cat. No. M9910
CDKI-73 Structure
Synonym:

CDKI73

Size Price Availability Quantity
2mg USD 261  USD290 In stock
5mg USD 382.5  USD425 In stock
10mg USD 549  USD610 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

CDKI-73 is a potent and orally active CDK9 inhibitor with Ki of 4 nM. CDKI-73 has Ki values of 4 nM, 4 nM and 3 nM for CDK9, CDK1 and CDK2, respectively. CDKI-73 shows selective toxicity to CLL cells (LD50=80 nM) versus normal B cell and normal CD34+ cell (LD50>20 uM). CDKI-73 induced caspase-dependent apoptosis that was preceded by dephosphorylation of cdk9 and serine 2 of RNA polymerase II. 

In vivo, CDKI-73 (25, 50, 100 mg/kg) markedly decreases tumor growth in a dose-dependent manner and results in a prolongation of animal life span (P < 0.001) without causing body weight loss and other overt toxicities.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 394.45
Formula C15H15FN6O2S2
CAS Number 1421693-22-2
Purity >99%
Solubility DMSO 40 mg/mL
Storage 2-8°C, dry, sealed
References

CDKI-73: an orally bioavailable and highly efficacious CDK9 inhibitor against acute myeloid leukemia
Muhammed H Rahaman, et al. Invest New Drυgs. 2019 Aug;37(4):625-635. PMID: 30194564.

Targeting RNA transcription and translation in ovarian cancer cells with pharmacological inhibitor CDKI-73
Frankie Lam, et al. Oncotarget. 2014 Sep 15;5(17):7691-704. PMID: 25277198.

A novel Cdk9 inhibitor preferentially targets tumor cells and synergizes with fludarabine
Elisabeth Walsby, et al. Oncotarget. 2014 Jan 30;5(2):375-85. PMID: 24495868.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: CDKI-73, CDKI73 supplier, CDK, inhibitors

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