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. Zotiraciclib inhibits cell proliferation concentrations in HCT-116 (IC50=0.079 μM) and HL-60 (IC50=0.059 μM).
In vivo, treatment with Zotiraciclib (SB1317) at 75 mg/kg po q.d. 3×/week significantly inhibits the growth of tumors with a mean TGI of 82%, while the lower dose of 50 mg/kg po 3×/week is marginally effective. Treatment with Zotiraciclib using either regime significantly inhibits the growth of tumors with mean TGIs of 42% and 63% for the oral and ip delivery methods, respectively.
|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 20 mg/mL|
 Anthony D William, et al. J Med Chem. Discovery of kinase spectrum selective macrocycle (16E)-14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo[126.96.36.199(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene (SB1317/TG02), a potent inhibitor of cyclin dependent kinases (CDKs), Janus kinase 2 (JAK2), and fms-like tyrosine kinase-3 (FLT3) for the treatment of cancer
|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.
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.
CDKI-73 is a potent and orally active CDK9 inhibitor with Ki of 4 nM.
THZ531 is a covalent CDK12 and CDK13 inhibitor with IC50 values of 158 nM and 69 nM, respectively.
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