Cimpuciclib tosylate

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CAS NO:	2408872-84-2
包装:	10mg
市场价:	11250元

产品介绍

Cimpuciclib tosylate 是一种选择性的 CDK4 抑制剂 (IC50: 0.49 nM)，具有抗肿瘤活性。

Cas No.

2408872-84-2

分子式

C₃₇H₄₃FN₈O₄S

分子量

714.85

溶解度

DMSO : 200 mg/mL (279.78 mM; Need ultrasonic)

储存条件

4°C, away from moisture

General tips

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.

Shipping Condition

Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

产品描述

Cimpuciclib tosylate is a selectiveCDK4inhibitor (IC₅₀: 0.49 nM) that has anti-tumor activity^[1].

Cimpuciclib (example 63, 141.2 nM, 6 days) tosylate inhibits proliferation of colo205 cells^[1].

Cell Proliferation Assay^[1]

Cell Line:	Colo205 cells
Concentration:	0-500 nM approximately
Incubation Time:	6 days
Result:	Inhibited cell proliferation with an IC₅₀value of 141.2 nM.

Cimpuciclib (example 63, 50 mg/kg, oral gavage, twice a week) tosylate inhibits tumor growth in colo205 tumor-bearing mice^[1].
Cimpuciclib (5 mg/kg for rats, 50 mg/kg for colo205 tumor-bearing mice, oral administration) tosylate shows slow metabolic rate and maintains high concentration in the plasma^[1].

Animal Model:	Colo205 tumor-bearing mice^[1]
Dosage:	50 mg/kg, twice a week
Administration:	Oral gavage
Result:	Inhibited tumor growth by 93.63%

Animal Model:

Rats, colo205 tumor-bearing mice^[1]

Dosage:

5 mg/kg for rats, 50 mg/kg for colo205 tumor-bearing mice.

Administration:

Oral administration

Result:

Pharmacokinetic profile of Cimpuciclib (example 63).

dose	C_max(ng/mL)	T_max(h)	AUC_0-24(ng/mL•h)	t_1/2(h)
5 mg/kg (rats)	559.7	6	5414	2.4
50 mg/kg (mice)	7960	1	136782	14.8