RET-IN-13

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

RET-IN-13 

RET-IN-13 (compound 1) 是一种喹啉化合物,一种有效的 RET 抑制剂,对 RET (WT) 和 RET (V804M) 的 IC50 分别为 0.5 nM 和 0.9 nM。RET-IN-13 具有用于与 RET 异常激活相关的肿瘤或肠道疾病研究的潜力。

RET-IN-13

RET-IN-13 Chemical Structure

CAS No. : 2684258-54-4

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生物活性

RET-IN-13 (compound 1), a quinoline compound, is a potent RET inhibitor with IC50s of 0.5 nM, 0.9 nM for RET (WT) and RET (V804M), respectively. RET-IN-13 has the potential for tumors or intestinal diseases related to abnormal activation of RET research[1].

体外研究
(In Vitro)

RET-IN-13 has low inhibition on CYP1A2 (IC50>50 μM), CYP2C9 (IC50=12.5 μM), CYP2C19 (IC50=16.9 μM), CYP2D6 (IC50=18.8 μM) and CYP3A4 (IC50>50 μM)[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

RET-IN-13 (compound 1; 0.5 mpk; iv) has a T1/2 of 6.93 hours, a CL of 2.68 mL/min·kg, and a Vdss of 1.52 L/kg for male mice[1].
RET-IN-13 (2.5 mpk; po) has a T1/2 of 5.16 hours, Cmax of 0.958 μM and an AUC of 12477 μM·hr for male mice[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

611.63

Formula

C32H33F4N5O3

CAS 号

2684258-54-4

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.

参考文献
  • [1]. Jiansong Wang, et al. Quinoline compounds. WO2021164742A1.

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