CDK4/6-IN-10 

CDK4/6-IN-10 is a potent, selective and orally active CDK4 and CDK6 inhibitor with IC₅₀s of 22 nM and 10 nM, respectively. CDK4/6-IN-10 shows antitumor activity. CDK4/6-IN-10 has the potential for the research of Multiple myeloma (MM)^[1].

CDK4/6-IN-10 (compouns 32) (1 µM) shows kinase selectivity with IC₅₀s of 22 nM and 10 nM for CDK4 and CDK6, respectively^[1].
CDK4/6-IN-10 (72 h) shows antiproliferative activity (GI₅₀s of 2.028, 5.802, 2.286, 2.238, 1.526, 11.381 µM for RPMI-8226, U266, K562, HL-60, 22RV1, HEK-293 cells, respectively)^[1].
CDK4/6-IN-10 (0, 1.5, 3, 6 µM, 24 h) induces cell cycle arrest at the G1 phase in a concentration-dependent manner^[1].
CDK4/6-IN-10 ( 0, 1, 2, 3 µM, 24 h) induces apoptosis of RPMI-8226 cells in a concentration-dependent manner^[1].
CDK4/6-IN-10 (0, 1.5, 3, 6 µM, 24 h) reduces the CDK4/6 activity by decreases the expression level of p-RB, c-MYC and BCL-2^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

CDK4/6-IN-10 (1000, 5000, 10000 mg/kg; p.o.) shows safety profile with LD₅₀ much higher than 10,000 mg/kg^[1].
CDK4/6-IN-10 (10 mg/kg; p.o.) shows oral bioavailability (F=51%) in SD rats^[1].
CDK4/6-IN-10 (100, 200 mg/kg; p.o., once a day for 19 days) shows antitumor potency and favorable safety profile^[1].
Pharmacokinetic Parameters of CDK4/6-IN-10 in SpragueeDawley rats^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

418.47

C₂₂H₂₃FN₈

2688098-11-3

CN1C=C(C2=NC(NC3=NC=C(CN4CCNCC4)C=C3)=NC=C2F)C5=CC=CN=C51

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Yuan K, et al. Discovery of novel and orally bioavailable CDK 4/6 inhibitors with high kinome selectivity, low toxicity and long-acting stability for the treatment of multiple myeloma. Eur J Med Chem. 2022; 228:114024.  [Content Brief]