PROTAC CDK12/13 Degrader-1

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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。

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品介绍

PROTAC CDK12/13 Degrader-1 (7f) 是一种高效选择性的细胞周期蛋白依赖性激酶CDK12/CDK13双重降解剂，其DC₅₀值分别是 2.2 nM 和 2.1 nM。PROTAC CDK12/13 Degrader-1 具有抗增殖活性，可用于乳腺癌的研究。

生物活性

PROTACCDK12/13 Degrader-1 (7f) is a highly selective cell cycle protein-dependent kinaseCDK12/CDK13dual degrader with theDC₅₀values of 2.2 nM and 2.1 nM, respectively.PROTACCDK12/13 Degrader-1 has anti-proliferative activity and can be used in breastcancerresearch^[1].

IC₅₀& Target^[1]

CDK12

2.2 nM (DC₅₀)

CDK13

2.1 nM (DC₅₀)

体外研究
(In Vitro)

PROTAC CDK12/13 Degrader-1 (7f) (0.02-10 μM, 150 h) significantly inhibits the proliferation of MFM223 and MDA-MB-231 cells in a dose-dependent manner^[1].
PROTAC CDK12/13 Degrader-1 (7f) (500 nM, 4 h) can significantly degrade CDK12 and CDK13 of MFM223 and MDA-MB-231 cells in a dose-dependent manner^[1].

Immunofluorescence^[1]

Cell Line:	MDA-MB-231 cell lines
Concentration:	1.0 μM
Incubation Time:	15 hours
Result:	Showed 88% degradation for CDK12 and 74% for CDK13. Acted on CDK12 with the DC₅₀value of 2.2 nM, and acted on CDK13 with the DC₅₀value of 2.1 nM.

体内研究
(In Vivo)

The pharmacokinetic parameters of PROTAC CDK12/13 Degrader-1 (7f) in rats^[1].

Parameters	oral (20 mg/kg)	iv (10 mg/kg)	ip (20mg/kg)	iv (2.5 mg/kg)
t_1/2(h)	-	5.28	10.85	5.8
T_max(h)	5.33	0.08	2.17	0.08
C_max(ng/mL)	7.73	19892.4	24.79	1498.5
C_max(ng/mL)	7.73	19892.4	24.79	1498.5
AUC_0-t(h*ng/mL)	21.83	7193.3	284.8	383.9
AUC_0-∞(h*ng/mL)	-	7242.7	318.5	391.55
CL (mL/h/kg)	-	1406.5	-	6495.4
F (%)	0.15	-	10.63	-

分子量

822.91

Formula

C₄₅H₄₆N₁₀O₆

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.