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ML 786 dihydrochloride Sale

目录号 : GC15296

Raf kinase inhibitor

ML 786 dihydrochloride Chemical Structure

Cas No.:1237536-18-3

规格 价格 库存 购买数量
10mg
¥3,959.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

IC50: 2.1, 2.5 and 4.2 nM for B-RafV600E, C-Raf and wild-type B-Raf, respectively

ML 786 is a potent Raf kinase inhibitor.

As one component of MAPK signal transduction pathway, the Raf isoform B-Raf has a high rate of activating mutation in melanoma (50-70%) and other cancers including papillary thyroid, ovarian, and colorectal. Inhibition of mutant B-Raf signaling, via either direct inhibition of the enzyme or inhibition of MEK, which is the direct substrate of Raf, has been demonstrated preclinically to inhibit tumor growth.

In vitro: ML 786 and its analog had been found to inhibit a significant number of kinases and were inhibitors of wild-type B-Raf and C-Raf. Although ML 786 and its analog displayed significant receptor tyrosine kinase activity, it was likely that such additional activity would not significantly contribute to pERK inhibition in melanoma tumors with constituitively activated B-Raf [1].

In vivo: ML 786 and its analog were found to have activity in vivo, as demonstrated by the fact that both compounds strongly inhibited the in vivo Raf pathway following a 75 or 100 mg/kg oral dose [1].

Clinical trial: N/A

Reference:
[1] Gould AE,Adams R,Adhikari S.  Design and optimization of potent and orally bioavailable tetrahydronaphthalene Raf inhibitors. J Med Chem.2011 Mar 24;54(6):1836-46.

Chemical Properties

Cas No. 1237536-18-3 SDF
化学名 (R,Z)-3-(2-aminopropan-2-yl)-N-(7-((7-hydroxy-5,6-dihydro-1,8-naphthyridin-4-yl)oxy)-1,2,3,4-tetrahydronaphthalen-2-yl)-5-(trifluoromethyl)benzimidic acid dihydrochloride
Canonical SMILES CC(C1=CC(C(F)(F)F)=CC(/C(O)=N/[C@]2([H])CCC3=CC=C(OC4=C5CCC(O)=NC5=NC=C4)C=C3C2)=C1)(N)C.Cl.Cl
分子式 C29H29F3N4O3.2HCl 分子量 611.48
溶解度 <61.15mg/ml in DMSO; <61.15mg/ml in Water 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.6354 mL 8.1769 mL 16.3538 mL
5 mM 0.3271 mL 1.6354 mL 3.2708 mL
10 mM 0.1635 mL 0.8177 mL 1.6354 mL
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