2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. BI-4142

BI-4142 是一种有效的、高选择性的、具有口服活性的 HER2 抑制剂，IC50 值为 5 nM。

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BI-4142 Chemical Structure

BI-4142 Chemical Structure

CAS No. : 2682003-36-5

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5 mg ￥5600
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Customer Review

BI-4142 相关抗体

Top Publications Citing Use of Products

查看 EGFR 亚型特异性产品:

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BI-4142 is a potent, highly selective and orally active HER2 inhibitor with an IC50 of 5 nM[1].

IC50 & Target

HER2

5 nM (IC50)

体外研究
(In Vitro)

BI-4142 shows inhibition with IC50 values of 10 nM, 18 nM, 270 nM and 2400 nM against HEK HER2YVMA, Ba/F3 HER2YVMA, HEK EGFRWT and Ba/F3 EGFRWT, respectively[1].
BI-4142 (1 nM-5 μM, 72 h or 96 h) shows antiproliferative activity against tumor cells[1].
BI-4142 displays good permeability and no PgP-mediated efflux liability in the CaCo-2 assay[1].
BI-4142 inhibits HER2-dependent cell lines and inhibits downstream signaling[1].

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

BI-4142 相关抗体:

Cell Proliferation Assay[1]

Cell Line: NCI-H2170 HER2WT, NCI-H2170 HER2YVMA, A431 EGFRWT, Ba/F3 HER2YVMA, Ba/F3 HER2YVMA,S783C, Ba/F3 EGFRWT and Ba/F3 EGFRC775S cells
Concentration: 1 nM-5 μM
Incubation Time: 72 h or 96 h
Result: Showed antiproliferative effect with IC50 values of 16 nM, 82 nM, >5 µM, 4 nM, 24 nM, 718 nM and 43 nM against NCI-H2170 HER2WT, NCI-H2170 HER2YVMA, A431 EGFRWT, Ba/F3 HER2YVMA, Ba/F3 HER2YVMA,S783C, Ba/F3 EGFRWT and Ba/F3 EGFRC775S, respectively.
体内研究
(In Vivo)

BI-4142 (0-100 mg/kg; p.o.; twice per day for 40 days) inhibits tumor growth and inhibits oncogenic signaling[1].

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

Animal Model: NMRI-Foxn1nu mice, PC-9 HER2YVMA xenograft model[1]
Dosage: 3, 10, 30 and 100 mg/kg
Administration: Oral administration, twice per day for 40 days
Result: Resulted in tumor regressions in a dose-dependent manner (113%, 126%, 153% and 166% tumor growth inhibition at 3, 10, 30 and 100 mg/kg, respectively).
Animal Model: BomTac:NMRI Foxn1nu mice[1]
Dosage: 1 mg/kg or 10mg/kg and 100 mg/kg
Administration: IV for 1 mg/kg, PO for 10mg/kg and 100 mg/kg (Pharmacokinetic Analysis)
Result: In vivo mouse PK data for BI-4142[1]
Compound Dose iv/po
(mg/kg)		 tmax
(h)		 Cmax
(nM)		 AUD
(h•nM)		 Plasma CL
(mL/min/kg)		 % F
i.v., 1mg/kg n/a n/a 3,280 9.69 n/a
BI-4142 p.o., 10 mg/kg 0.83 8,600 23,200 n/a 71
p.o., 100 mg/kg 0.67 36,400 196,000 n/a 60
分子量

521.57

Formula

C28H27N9O2
CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 100 mg/mL (191.73 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)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9173 mL 9.5864 mL 19.1729 mL
5 mM 0.3835 mL 1.9173 mL 3.8346 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, 6 months; -20°C, 1 month (protect from light)。-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。

  • 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

只
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: 98.39%

COA (261 KB) LCMS (173 KB)

产品使用指南 (1538 KB)
参考文献

BI-4142 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, 6 months; -20°C, 1 month (protect from light)。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9173 mL 9.5864 mL 19.1729 mL 47.9322 mL
5 mM 0.3835 mL 1.9173 mL 3.8346 mL 9.5864 mL
10 mM 0.1917 mL 0.9586 mL 1.9173 mL 4.7932 mL
15 mM 0.1278 mL 0.6391 mL 1.2782 mL 3.1955 mL
20 mM 0.0959 mL 0.4793 mL 0.9586 mL 2.3966 mL
25 mM 0.0767 mL 0.3835 mL 0.7669 mL 1.9173 mL
30 mM 0.0639 mL 0.3195 mL 0.6391 mL 1.5977 mL
40 mM 0.0479 mL 0.2397 mL 0.4793 mL 1.1983 mL
50 mM 0.0383 mL 0.1917 mL 0.3835 mL 0.9586 mL
60 mM 0.0320 mL 0.1598 mL 0.3195 mL 0.7989 mL
80 mM 0.0240 mL 0.1198 mL 0.2397 mL 0.5992 mL
100 mM 0.0192 mL 0.0959 mL 0.1917 mL 0.4793 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.

Keywords:

BI-41422682003-36-5BI4142BI 4142EGFREpidermal growth factor receptorErbB-1HER1HEKBa/F3PC-9antitumorInhibitorinhibitorinhibit

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目录号：
HY-150024
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