Abemaciclib (LY2835219) is a potent and selective inhibitor for CDK4 and CDK6 with IC50 values of 2 nM and 10 nM, respectively. LY2835219 reduces cell viability with the IC50 values ranging from 0.5 μM to 0.7 μM, inhibits Akt and ERK signaling but not mTOR activation at head and neck squamous cell carcinoma (HNSCC) cells. LY2835219 shows inhibition on A375R1-4, M14R, and SH4R with EC50 values ranging from 0.3 to 0.6 μM. Abemaciclib (LY2835219) inhibits the proliferation of the parental A375 and resistant A375RV1 and A375RV2 cells with similar potencies with IC50 values of 395, 260, and 463 nM, respectively.
In vivo, Abemaciclib (45 mg/kg, p.o.) in combination with RAD001 causes a cooperative antitumor effect in HNSCC xenograft tumor. Abemaciclib (45 or 90 mg/kg, p.o.) shows significant tumor growth inhibition in an A375 xenograft model.
|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 5 mg/mL|
|Storage||2-8°C, protect from light, sealed|
The CDK4/6 inhibitor LY2835219 has potent activity in combination with mTOR inhibitor in head and neck squamous cell carcinoma
Bo Mi Ku, et al. Oncotarget. 2016 Mar 22;7(12):14803-13. PMID: 26909611.
The CDK4/6 inhibitor LY2835219 overcomes vemurafenib resistance resulting from MAPK reactivation and cyclin D1 upregulation
Vipin Yadav, et al. Mol Cancer Ther. 2014 Oct;13(10):2253-63. PMID: 25122067.
Preclinical characterization of the CDK4/6 inhibitor LY2835219: in-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with gemcitabine
Lawrence M Gelbert, et al. Invest New Drugs. 2014 Oct;32(5):825-37. PMID: 24919854.
|Related CDK Products|
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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.
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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