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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO 40 mg/mL|
|Storage||2-8°C, dry, sealed|
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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SR-4835 is a highly selective, dual inhibitor of CDK12 with IC50 values of 99 nM, Kd of 98 nM and CDK13 with Kd of 4.9 nM, respectively.
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