aladdin 阿拉丁 C413825 CCT196969 1163719-56-9 98%

中文名：CCT196969

英文名：CCT196969

纯度：Moligand™，≥98%

货号：C413825

Cas号：1163719-56-9

存储温度：-20°C储存

运输条件：超低温运输

产品介绍：

Information

CCT196969 is a novel orally available, pan-RAFinhibitor with anti-SRCactivity. It also inhibits SRC, LCK, and the p38 MAPKs.

Targets

CRAF (Cell-free assay); LCK (Cell-free assay); Src (Cell-free assay); V600E-BRAF (Cell-free assay); BRAF (Cell-free assay) ;0.01 μM; 0.02 μM; 0.03 μM; 0.04 μM; 0.1 μM

In vitro

CCT196969 is active against melanoma and colorectal cancer cell lines that are mutant for BRAF, but not cancer cells that are wild-type for BRAF and NRAS. CCT196969 induces caspase 3 and PARP cleavage, thus induces apoptosis. CCT196969 does not drive paradoxical pathway activation and inhibit MEK/ERK in BRAF and NRAS mutant melanoma.

In vivo

CCT196969 is extremely well tolerated at the doses assessed and does not produce any significant adverse effects in vivo. Oral dosing at 10 mg/kg/day of CCT196969 results in plasma concentrations ∼1 μM at 24 hr. It is orally bioavailable at ∼55%.

Cell Research(from reference)

Cell lines：cell line derived from a vemurafenib-resistant melanoma 

Concentrations：1 μM 

Incubation Time：4 h 

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