RET-IN-20

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RET-IN-20

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

RET-IN-20 是一种有效的RET抑制剂，IC₅₀值为 13.7 nM。RET-IN-20 降低 p-Ret、p-Shc 蛋白的表达。RET-IN-20 诱导细胞凋亡 (apoptosis)。RET-IN-20 具有抗增殖和抗肿瘤活性。

生物活性

RET-IN-20 is a potentRETinhibitor with anIC₅₀value of 13.7 nM. RET-IN-20 decreases the expression of p-Ret, p-Shc protein. RET-IN-20 inducesapoptosis. RET-IN-20 shows antiproliferative and anti-tumor activity^[1].

IC₅₀& Target

IC₅₀: 3.7 nM (RET)^[1]

体外研究
(In Vitro)

RET-IN-20 (compound 8q) (0, 1.2, 3.7, 11.1, 33.3, 100 nM; 4 h) 以剂量依赖性方式降低 p-Ret、p-Shc 蛋白的表达^[1]。
RET-IN-20 (0, 33.3, 100, 300 nM; 48 h) 以剂量依赖的方式诱导细胞凋亡^[1]。

Cell Proliferation Assay^[1]

Cell Line:	Ba/F3 RET^WT, Ba/F3 RET^V804M, Ba/F3 RET^G810C, Ba/F3 RET^G810R, Ba/F3 parental cells
Concentration:	0-10000 nM
Incubation Time:	72 h
Result:	Showed antiproliferative activities with IC₅₀s of 5.6, 24.4, 15.4, 53.2, >10000 nM for Ba/F3 RET^WT, Ba/F3 RET^V804M, Ba/F3 RET^G810C, Ba/F3 RET^G810R, Ba/F3 parental, respectively.

Apoptosis Analysis^[1]

Cell Line:	CCDC6-RET-WT, CCDC6-RET-V804M, CCDC6-RET-G810C, CCDC6-RET-G810R cells
Concentration:	0, 1.2, 3.7, 11.1, 33.3, 100 nM
Incubation Time:	4 h
Result:	Inhibited the expression of p-Ret, p-Shc protein in a dose dependent manner.

Western Blot Analysis^[1]

Cell Line:	Ba/F3-CCDC6-RET^{G810 C/R}cells
Concentration:	0, 33.3, 100, 300 nM
Incubation Time:	48 h
Result:	Induced approximately 53.40% and 32.67% of cells undergoing apoptosis at a concentration of 300 nM in Ba/F3-CCDC6-RET^G810Cand Ba/F3-CCDC6-RET^G810Rcells, respectively.

体内研究
(In Vivo)

RET-IN-20 (10, 30 mg/kg; i.p.; once a day for 13 continuous days) 在小鼠体内显示出抗肿瘤活性^[1]。

Animal Model:	CB17-SCID mice (Ba/F3-CCDC6-RETG810C tumor)^[1]
Dosage:	10, 30 mg/kg
Administration:	I.p.; once a day for 13 continuous days
Result:	Suppressed tumor growth in a dose-dependent manner with tumor growth inhibition values (TGI) of 17.1% and 66.9%, respectively.

分子量

584.64

Formula

C₃₂H₃₃FN₆O₄

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.