PROTAC CDK12/13 Degrader-1|西域试剂

PROTAC CDK12/13 Degrader-1

产品编号：Bellancom-151110| 分子式：C₄₅H₄₆N₁₀O₆| 分子量：822.91

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货号	价格	库存与货期
Bellancom-151110	￥3500.00	杭州北京（现货）
Bellancom-151110	￥8500.00	杭州北京（现货）
Bellancom-151110	￥13500.00	杭州北京（现货）

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PROTAC CDK12/13 Degrader-1

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

PROTAC CDK12/13 Degrader-1 (7f) is a highly selective cell cycle protein-dependent kinase CDK12/CDK13 dual degrader with the DC₅₀ values of 2.2 nM and 2.1 nM, respectively. PROTAC CDK12/13 Degrader-1 has anti-proliferative activity and can be used in breast cancer research.

体外研究

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.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Immunofluorescence

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 DC₅₀ value of 2.2 nM, and acted on CDK13 with the DC₅₀ value of 2.1 nM.

体内研究
(In Vivo)

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

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	-

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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

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	-

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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

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	-