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CCT241161
本半岛bd体育手机客户端 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。
CCT241161图片
CAS NO: 1163719-91-2
包装与价格：
包装 价格(元)
100mg 电议
250mg 电议
500mg 电议

半岛bd体育手机客户端 介绍
CCT241161 是一种口服有效的泛型 RAF抑制剂，其对 LCK, CRAF, SRC, V600E-BRAF和 BRAF的 IC50值分别为 3, 6, 10, 15 和 30 nM。CCT241161 对 BRAF和 NRAS突变的黑色素瘤具有良好的活性。CCT241161 还具有抗癌细胞增殖活性。
生物活性

CCT241161 is an orally active pan-RAFinhibitor withIC50s of 3, 6, 10, 15 and 30 nM forLCK,CRAF,SRC,V600E-BRAFandBRAF, respectively. CCT241161 shows good activity to inBRAFandNRASmutant melanomas. CCT241161 also exhibits anticancer cell proliferative activity[1].
IC50& Target

CRAF

6 nM (IC50)

Braf

30 nM (IC50)

BRafV600E

15 nM (IC50)

SRC

0.01 μM (IC50)

LCK

0.003 μM (IC50)
体外研究
(In Vitro)

CCT241161 (1, 3, 10, 30, 100 nM; 24 h) inhibits MEK and ERK in WM266.4 cells[1].
CCT241161 (1, 10, 100 nM and 1, 10, 100 μM) inhibits BRAFV600Ein Ba/F3 cells[1].
CCT241161 (0.5 μM; 20 days) inhibits A375 cell but not cause drug resistance[1].
CCT241161 (1 μM , 4 h) inhibits BRAF-inhibitor-resistant melanoma cells[1].
CCT241161 (0.1, 0.3, 1, 3, 10 μM; 24 h) inhibits MEK in NRAS mutant cells[1].
CCT241161 (0.1, 1, 10, 100 μM) shows anti-proliferative activity in D04 cells[1].

Cell Viability Assay[1]

Cell Line: WM266.4 cells (BRAF mutant)
Concentration: 1, 3, 10, 30, 100 nM
Incubation Time: 24 h
Result: Exhibited effects of inhibiting MEK and ERK in WM266.4 cells.

Cell Viability Assay[1]

Cell Line: Ba/F3 cells
Concentration: 1, 10, 100 nM and 1, 10, 100 μM
Incubation Time:
Result: Inhibited BRAF-V600E and BRAF-T529N, V600E in Ba/F3 cells.

Cell Viability Assay[1]

Cell Line: A375 cell
Concentration: 0.5 μM
Incubation Time: 20 days
Result: Maintained inhibitory activity against A375 cell ,without drug resistance in 20 days.

Cell Proliferation Assay[1]

Cell Line: D04 cells
Concentration: 0.1, 1, 10, 100 μM
Incubation Time:
Result: Efficiently inhibited NRAS mutant cell growth.

Western Blot Analysis[1]

Cell Line: patient #2 (PLX4720-resistant cells from patient with vemurafenib-resistant melanoma)
Concentration: 1 μM
Incubation Time: 4 h
Result: Inhibited MEK, ERK, and SRC in the cells from patient #2.

Western Blot Analysis[1]

Cell Line: D04 cells
Concentration: 0.1, 0.3, 1, 3, 10 μM
Incubation Time: 24 h
Result: Showed activity of surpressing MEK in NRAS mutant cells.
体内研究
(In Vivo)

CCT241161 (10, 20 mg/kg; i.g; once a day for 7 days) inhibits the growth of BRAF mutant A375, PLX4720-resistant A375 and NRAS mutant DO4 tumor xenografts in mice[1].

Animal Model: Female nude mice (5 to 6- week-old)[1].
Dosage: 10, 20 mg/kg
Administration: Oral gavage; once a day for 7 days.
Result: Showed activity of tumor regression in nude mice with xenografts tumor of BRAF mutant A375, PLX4720-resistant A375 (A375/R) and NRAS mutant DO4, without causing any body weight loss to the mice.
分子量

541.62
Formula

C28H27N7O3S
CAS 号

1163719-91-2
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.
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