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CDK4/6-IN-10
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
CDK4/6-IN-10图片
CAS NO:2688098-11-3
包装与价格：
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
CDK4/6-IN-10 是一种有效的、选择性的和具有口服活性的CDK4和CDK6抑制剂，其IC50值分别为 22 nM 和 10 nM。CDK4/6-IN-10 显示出抗肿瘤活性。CDK4/6-IN-10 具有研究多发性骨髓瘤 (MM) 的潜力。
生物活性

CDK4/6-IN-10 is a potent, selective and orally activeCDK4andCDK6inhibitor withIC50s 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].

IC50& Target[1]

CDK4

22 nM (IC50)

CDK6/cyclinD1

10 nM (IC50)

体外研究
(In Vitro)

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].

Cell Proliferation Assay[1]

Cell Line:RPMI-8226, U266, K562, HL-60, 22RV1, HEK-293 cells
Concentration:
Incubation Time:72 h
Result: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).

Cell Cycle Analysis[1]

Cell Line:RPMI-8226 cells
Concentration:0, 1.5, 3, 6 μM
Incubation Time:24 h
Result:Cells were arrested at the G1 phase in a concentration-dependent manner.

Apoptosis Analysis[1]

Cell Line:RPMI-8226 cells
Concentration:0, 1.5, 3, 6 μM
Incubation Time:24 h
Result:Reduced the CD4/K activity by decreased the expression level of p-RB, c-MYC and BCL-2.
体内研究
(In Vivo)

CDK4/6-IN-10 (1000, 5000, 10000 mg/kg; p.o.) shows safety profile with LD50much 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].

CompdAdmin.Cmax(ng/mL)AUC0-t(h·ng/mL)MRT0-t(h)Tmax(h)t1/2(h)CL (mL/h/kg)F (%)
32i.v.3559605.90.0338.9641-
p.o.2574,87812.810.7>2452451
SpragueeDawley rats, 10 mg/kg, p.o.

Animal Model:ICR mice[1]
Dosage:1000, 5000, 10000 mg/kg
Administration:p.o.
Result:Showed safety profile with LD50much higher than 10,000 mg/kg.
Animal Model:SpragueeDawley rats[1]
Dosage:10 mg/kg
Administration:p.o.
Result:Showed oral bioavailability (F=51%).
Animal Model:BALB/c nude mice (6-8 weeks) (MM xenograft model)[1]
Dosage:100, 200 mg/kg
Administration:p.o., once a day, 19 days
Result:Showed antitumor potency and favorable safety profile.
分子量

418.47

Formula

C22H23FN8

CAS 号

2688098-11-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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