CCT196969
目录号: PL10779 纯度: ≥99%
CAS No. :1163719-56-9
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中文名称
CCT196969
中文别名
N-[4-[(3,4-二氢-3-氧代吡啶并[2,3-b]吡嗪-8-基)氧基]-2-氟苯基]-N'-[3-(1,1-二甲基乙基)-1-苯基-1H-吡唑-5-基]脲;CCT196969
英文名称
CCT196969
英文别名
CCT196969;1-(3-(tert-butyl)-1-phenyl-1H-pyrazol-5-yl)-3-(2-fluoro-4-((3-oxo-3,4-dihydropyrido[2,3-b]pyrazin-8-yl)oxy)phenyl)urea;1-(5-tert-butyl-2-phenylpyrazol-3-yl)-3-[2-fluoro-4-[(3-oxo-4H-pyrido[2,3-b]pyrazin-8-yl)oxy]phenyl]urea;GTPL9815;BCP19551;BDBM50457449;s7743;1-(3-(t-Butyl)-1-phenyl-1H-pyrazol-5-yl)-3-(2-fluoro-4-((3-oxo-3,4-dihydropyrido[2,3-b]pyrazin-8-yl
Cas No.
1163719-56-9
分子式
C27H24FN7O3
分子量
513.52
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
CCT196969 是一种泛-Raf 抑制剂,抑制 B-Raf,BRafV600E 和 CRAF,IC50 分别为 0.1, 0.04, 和 0.01 μM。
生物活性
CCT196969 is a pan-Raf inhibitor, which inhibits B-Raf, BRaf and CRAF with IC 50 s of 0.1, 0.04, and 0.01 μM, respectively.
性状
Solid
IC50 & Target[1][2]
BRaf 0.04 μM (IC50) Braf 0.1 μM (IC50
体外研究(In Vitro)
CCT196969 is a pan-Raf inhibitor with anti-SRC activity. CCT196969 is an orally available, well-tolerated B-Raf inhibitor that directly inhibits B-Raf in cells. CCT196969 inhibits B-Raf at 100 nM and B-Raf at 40 nM. It inhibits CRaf at 12 nM, SRC at 26 nM, and LCK at 14 nM. CCT196969 is active against melanoma and colorectal cancer cell lines that are mutant for B-Raf. CCT196969 induces caspase 3 and PARP cleavage, demonstrating that it induces apoptosis. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
CCT196969 is extremely well tolerated and does not produce any significant adverse effects in vivo. It inhibits the growth of NRAS mutant DO4 tumor xenografts in nude mice. CCT196969 inhibits ERK and SRC and induce tumor regression in a PDX from the resistant tumor without causing body weight loss in the mice. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Girotti MR, et al. Paradox-breaking RAF inhibitors that also target SRC are effective in drug-resistant BRAF mutant melanoma. Cancer Cell. 2015 Jan 12;27(1):85-96.
溶解度数据
In Vitro: DMSO : ≥ 32 mg/mL (62.32 mM)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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