1. MAPK/ERK Pathway
  2. Raf
  3. BI-882370

BI-882370 是一种高效选择性的 RAF 激酶抑制剂,其结合位于 BRAF 激酶的 DFG-out 无活性构象处 (ATP 结合位点)。 BI-882370 抑制 BRAFV600E-mutant, WT BRAF 和 CRAF 激酶的 IC50 值分别为 0.4,0.8 和 0.6 nM。BI-882370 也可以抑制 SRC 家族激酶。

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BI-882370 Chemical Structure

BI-882370 Chemical Structure

CAS No. : 1392429-79-6

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1 mg ¥431
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5 mg ¥950
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10 mg ¥1700
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50 mg ¥5500
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100 mg ¥9700
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Customer Review

查看 Raf 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BI-882370 is a potent and selective RAF kinase inhibitor that binds to the ATP binding site of the kinase positioned in the DFG-out (inactive) conformation of the BRAF kinase. BI-882370 (BI 882370) inhibits the oncogenic BRAFV600E-mutant, the WT BRAF and CRAF kinases with IC50s of 0.4, 0.8, and 0.6 nM, respectively. BI-882370 also inhibits SRC family kinases[1].

IC50 & Target[1]

Braf

0.6 nM (IC50)

c-Raf

0.8 nM (IC50)

BRafV600E

0.4 nM (IC50)

体外研究
(In Vitro)

BI-882370 (0.9-6000 nM; 3 days) inhibits the BRAF-mutant human melanoma and colorectal cancer cells proliferation with a EC50 range of 1-10 nM[1].
BI 882370 (0.1-100 nM, 0.1-3000 nM; 2 hours) results in a reduction of p-MEK1/2, p-ERK1/2 and cyclin D1/D2 expression in BRAFV600E-mutant A375 cells; induces phosphorylation of MEK1/2 and enhanced phosphorylation of ERK1/2 in WT BRO cells (3-300 nM)[1].
BI 882370 (0.1-100 nM, 0.1-3000 nM; 24 hours) suppresses cyclin D1/D2 expression, induces Kip1/p27 expression at concentrations of 1 nM or higher in BRAFV600E-mutant A375 cells, expression of cyclins D1/D2 or Kip1/p27 is not affected in WT BRO cells[1].

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

Cell Proliferation Assay[1]

Cell Line: BRAF-mutant and WT melanoma cell lines (A101D, A375, SK-MEL-28, G-361, and BRO); Colorectal cancer cell lines (COLO 205, HT-29, LS411N, and HCT-116)
Concentration: 0.9-6000 nM
Incubation Time: 3 days
Result: Showed a EC50 range of 1-10 nM in an extended panel of BRAF-mutant human melanoma and colorectal cancer cell; while proliferation of BRAF WT cells was inhibited with EC50 >1 μM.

Western Blot Analysis[1]

Cell Line: BRAFV600E-mutant A375 cells; BRAF WT, NRAS-mutant BRO (WT BRO) cells
Concentration: 0.1-100 nM; 0.1-3000 nM
Incubation Time: 2 hours; 24 hours
Result: Resulted in a reduction of phospho-MEK1/2 signals and cyclin D1/D2 expression in BRAFV600E-mutant A375 cells.
体内研究
(In Vivo)

BI-882370 (deliver orally; 25 mg/kg, 50 mg/kg; twice daily; 2 weeks) is efficacious in multiple mouse models of BRAF-mutant melanomas and colorectal carcinomas, shows superior efficacy compared with Vemurafenib, Dabrafenib, or Trametinib[1].
BI-882370 (deliver orally; 25 mg/kg; twice daily; 40 days) developes resistance within 3 weeks, but resistance is not observed during 5 weeks of second-line therapy in combination with trametinib[1].
BI-882370 (deliver orally; 60 mg/kg; once daily; 2 weeks) indicates lack of toxicity in terms of clinical chemistry, hematology, pathology, and toxicogenomics in rats[1].

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

Animal Model: Human melanoma xenografts in nude mice with BRAF-mutant melanomas and colorectal carcinomas cells (A375, COLO 205; G-361, HT-29 cells)[1]
Dosage: 25 mg/kg; 50 mg/kg
Administration: Deliver orally; 25 mg/kg, 50 mg/kg; twice daily; 2 weeks
Result: Regressed tumors partially, upon discontinuation, tumor regrowth was markedly delayed.
分子量

569.67

Formula

C28H33F2N7O2S

CAS 号
性状

固体

颜色

Off-white to gray

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
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 17.86 mg/mL (31.35 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7554 mL 8.7770 mL 17.5540 mL
5 mM 0.3511 mL 1.7554 mL 3.5108 mL
查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.16%

参考文献

BI-882370 相关分类

完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7554 mL 8.7770 mL 17.5540 mL 43.8851 mL
5 mM 0.3511 mL 1.7554 mL 3.5108 mL 8.7770 mL
10 mM 0.1755 mL 0.8777 mL 1.7554 mL 4.3885 mL
15 mM 0.1170 mL 0.5851 mL 1.1703 mL 2.9257 mL
20 mM 0.0878 mL 0.4389 mL 0.8777 mL 2.1943 mL
25 mM 0.0702 mL 0.3511 mL 0.7022 mL 1.7554 mL
30 mM 0.0585 mL 0.2926 mL 0.5851 mL 1.4628 mL
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.

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目录号:
HY-107779
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