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|
|Related CDK Products|
Abemaciclib (LY2835219) is a potent and selective inhibitor for CDK4 and CDK6 with IC50 values of 2 nM and 10 nM, respectively.
Zotiraciclib (TG02, SB1317) is an orally bioavailable, brain penetrant multi-kinase inhibitor of CDK2, JAK2, and FLT3 with IC50 values of 13, 73, and 56 nM, respectively.
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.
Trilaciclib (G1T28) is a potent first-in-class reversible CDK4/6 inhibitor with IC50 of 1 nM and 4 nM for CDK4/cyclin D1 and CDK6/cyclin D3, respectively.
THZ531 is a covalent CDK12 and CDK13 inhibitor with IC50 values of 158 nM and 69 nM, respectively.
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