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CDK4/6-IN-14
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-14图片
CAS NO:2699091-15-9
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-14 是一种有效且高度选择性的CDK4CDK6(CDK) 抑制剂,IC50分别为 10 nM 和 16 nM。CDK4/6-IN-14 的选择性是 CDK 1、2、7 和 9 的 60 多倍,并且在其他 205 种激酶中表现出高选择性。
生物活性

CDK4/6-IN-14 is a potent and highly selectiveCDK4andCDK6(CDK) inhibitor withIC50s of 10 nM and 16 nM, respectively. CDK4/6-IN-14 exhibits more than 60-fold selectivity over CDKs 1, 2, 7, and 9, and shows high selectivity among other 205 kinases[1].

IC50& Target[1]

CDK4

10 nM (IC50)

CDK6

16 nM (IC50)

CDK1

>10000 nM (IC50)

CDK2

1045 nM (IC50)

CDK7

2595 nM (IC50)

CDK9

2664 nM (IC50)

体外研究
(In Vitro)

CDK4/6-IN-14 (compound 42; 1-6 μM; 5 days) exhibits potent inhibitory activity against the proliferation of breast cancer MCF-7, T47D, and ZR-75-1 cell lines. CDK4/6-IN-14 significantly inhibits growth and clone formation of MCF-7 and T47D cells[1].
CDK4/6-IN-14 (compound 42; 1-6 μM) arrests the cell cycle at the G1 phase of MCF-7 and T47D cells in the dose-dependent manner[1].
CDK4/6-IN-14 (compound 42; 1-6 μM; 24 hours) significantly inhibits the phosphorylation of retinoblastoma (RB), while the expression of RB protein was almost unchanged. In addition, CDK4/6-IN-14 exhibits a concentration-dependent effect to decrease the level of c-MYC and cyclin D1[1].

Cell Cytotoxicity Assay[1]

Cell Line:MCF-7 and T47D cells
Concentration:1 μM, 2 μM, 4 μM (T47D cells); 1.5 μM, 3 μM, 6 μM (MCF-7 cells)
Incubation Time:5 days
Result:Significantly inhibited growth and clone formation of MCF-7 and T47D cells.

Western Blot Analysis[1]

Cell Line:MCF-7 and T47D cells
Concentration:1 μM, 2 μM, 4 μM (T47D cells); 1.5 μM, 3 μM, 6 μM (MCF-7 cells)
Incubation Time:24 hours
Result:Significantly inhibited the phosphorylation of RB.
体内研究
(In Vivo)

CDK4/6-IN-14 (compound 42; 100-150 mg/kg; p.o; once a day; for 23 days) significantly inhibits tumor growth of the MCF-7 xenograft model[1].
CDK4/6-IN-14 (compound 42) exhibits a suitable t1/2 of intravenous and oral administration (2.62 and 3.59 h, respectively). Moreover, the oral bioavailability of CDK4/6-IN-14 is 43%[1].
Pharmacokinetic Parameters of CDK4/6-IN-14 (Compound 42) in Sprague–Dawley Rats[1].

admin.Cmax(ng/mL)AUC0-∞(h × ng/mL)MRT0-∞(h)Tmax(h)t1/2(h)F (%)
IV290.52372.563.500.0332.62
PO144.111612.189.1163.5943
Dose: i.v. at 1 mg/kg; p.o. at 10 mg/kg[1]

Animal Model:BALB/c nude mice bearing MCF-7 cells[1]
Dosage:100 mg/kg, 150 mg/kg
Administration:Orally administertion; once a day; for 23 days
Result:Significantly inhibited tumor growth of the MCF-7 xenograft model.
分子量

483.97

Formula

C24H27ClFN7O

CAS 号

2699091-15-9

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.