2. MAPK/ERK Pathway Protein Tyrosine Kinase/RTK
  3. Raf Bcr-Abl Discoidin Domain Receptor VEGFR RET Ephrin Receptor
  4. ML786 dihydrochloride

ML786 dihydrochloride 是一种有效和具有口服活性的 Raf 抑制剂，对 V600EΔB-Raf，wt B-Raf 和 C-Raf 的 IC50 值分别为2.1，4.2 和 2.5 nM。ML786 dihydrochloride 还抑制 Abl-1，DDR2，EPHA2，KDR 和 RET (IC50=<0.5, 7.0, 11, 6.2, 0.8 nM)。ML786 dihydrochloride 可用于癌症研究。

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ML786 dihydrochloride Chemical Structure

ML786 dihydrochloride Chemical Structure

CAS No. : 1237536-18-3

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Other Forms of ML786 dihydrochloride:

ML786 dihydrochloride 相关抗体

Top Publications Citing Use of Products

查看 Raf 亚型特异性产品:

查看所有亚型
BRaf c-Raf Raf

查看 Discoidin Domain Receptor 亚型特异性产品:

查看所有亚型
DDR1 DDR2

查看 VEGFR 亚型特异性产品:

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

查看 Ephrin Receptor 亚型特异性产品:

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EphA2 EphA3 EphA4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ML786 dihydrochloride is a potent and orally bioavailable Raf inhibitor, with IC50s of 2.1, 4.2, and 2.5 nM for V600EΔB-Raf, wt B-Raf, and C-Raf, respectively. ML786 dihydrochloride also inhibits Abl-1, DDR2, EPHA2, KDR, and RET (IC50=<0.5, 7.0, 11, 6.2, 0.8 nM). ML786 dihydrochloride can be used for the research of cancers[1].

IC50 & Target[1]

RAF

2.1 nM (IC50)

Abl1

<0.5 nM (IC50)

DDR2

7.0 nM (IC50)

KDR

6.2 nM (IC50)

EPHA2

11 nM (IC50)

RET

0.8 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A-375 IC50
56 nM
Compound: 6
Inhibition of B-Raf V600E mutant in human A375 cell line assessed as inhibition of ERK phosphorylation for 3 hrs with compound by ELISA
Inhibition of B-Raf V600E mutant in human A375 cell line assessed as inhibition of ERK phosphorylation for 3 hrs with compound by ELISA
[PMID: 26804230]
体外研究
(In Vitro)

ML786 (3 小时) 抑制 A375 细胞中细胞外信号调节激酶 (ERK) (pERK) 的激酶磷酸化，IC50 为 60 nM[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

ML786 dihydrochloride 相关抗体:
体内研究
(In Vivo)

ML786 (75 mg/kg；口服，每日一次，共 21 天) 可抑制免疫功能低下小鼠的皮下 A375 M 异种移植[1]。
ML786 (75 mg/kg；单次口服) 可强烈抑制小鼠的 Raf 通路[1]。
ML786 (10 mg/kg；口服) 在大鼠中的口服生物利用度为 85%，AUC1-24h 为 35.9 μM·h[1]。
ML786 (1 mg/kg；静脉注射) 在大鼠中的血浆清除率为 0.44 L/h/kg，Vss 为 3.93 L/kg[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Nude NCR (ν/ν) mice bearing A375 M xenografts[1]
Dosage: 75 mg/kg
Administration: P.o. once daily for 21 days
Result: Induced partial regressions of the tumor xenografts.
Showed no indication of toxicity or weight loss.
分子量

611.48

Formula

C29H31Cl2F3N4O3
CAS 号
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.
纯度 & 产品资料
参考文献

ML786 dihydrochloride 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ML7861237536-18-3ML 786ML-786RafBcr-AblDiscoidin Domain ReceptorVEGFRRETEphrin ReceptorRaf kinasesVascular endothelial growth factor receptorB-RafC-RafAbl-1DDR2EPHA2KDRcancerInhibitorinhibitorinhibit

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产品名称：
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目录号：
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