2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR Cell Cycle/DNA Damage MAPK/ERK Pathway Epigenetics Stem Cell/Wnt
  3. EGFR Itk PI4K Btk CDK Raf JAK
  4. BI-1622

BI-1622 是一种口服有效的和高选择性 HER2 (ERBB2) 抑制剂，IC50 为 7 nM。BI-1622对 EGFR 的选择性大于 25 倍。BI-1622 在转染 H2170 和 PC9 细胞的移植瘤小鼠模型中表现出较高的体内的抗肿瘤效果，具有良好的活性分子代谢和药代动力学特性。

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BI-1622 Chemical Structure

BI-1622 Chemical Structure

CAS No. : 2681392-19-6

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥4139
In-stock
1 mg ￥1500
In-stock
5 mg ￥3700
In-stock
10 mg ￥6000
In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Customer Review

BI-1622 相关抗体

Top Publications Citing Use of Products

查看 EGFR 亚型特异性产品:

查看所有亚型
EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

查看 PI4K 亚型特异性产品:

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PI4KIIIβ PI4KIIIα PI4K PI4KII

查看 CDK 亚型特异性产品:

查看所有亚型
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

查看 Raf 亚型特异性产品:

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BRaf c-Raf Raf

查看 JAK 亚型特异性产品:

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JAK1 JAK2 JAK3 Tyk2 JAK

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BI-1622 is an orally active, potent and highly selective HER2 (ERBB2) inhibitor, with an IC50 of 7 nM. BI-1622 shows greater than 25-fold selectivity over EGFR. BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models with engineered H2170 and PC9 cells and had a favorable agent metabolism and pharmacokinetics profile[1].

IC50 & Target

HER2

7 nM (IC50)

ErbB4

 

EGFR

 

CDK11B

 

JAK3

 

体外研究
(In Vitro)

BI-1622 (0-5 µM, 72 h or 96 h) inhibits the proliferation of HER2-dependent cell lines[1].
BI-1622 induces a dose-dependent decrease in pHER2 and pERK levels in NCI-H2170 HER2YVMA and PC-9 HER2YVMA cells with an accompanying decrease in DUSP6 messenger RNA levels[1].
BI-1622 displays good permeability and no PgP-mediated efflux liability[1].
BI-1622 shows good in vitro clearance in mouse liver microsomes and mouse hepatocytes[1].

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

BI-1622 相关抗体:

Cell Proliferation Assay[1]

Cell Line: Ba/F3 cells
Concentration: 0-5 µM
Incubation Time: 72 h or 96 h
Result: Potently inhibited the proliferation of cancer cell lines dependent on amplified HER2 or an NRG-1 fusion. Inhibited different HER2 oncogenic variants and HER2WT with IC50 values below 50 nM in tumor cell lines, while sparing EGFRWT-driven cells.
体内研究
(In Vivo)

BI-1622 (1 mg/kg, IV; 10 and 100 mg/kg, Orally; once) shows moderate clearance, a moderate volume of distribution, and good to moderate bioavailability[1].
BI-1622 (0-100 mg/kg, orally, twice daily) inhibits tumor growth and inhibits oncogenic signaling in vivo[1].

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

Animal Model: Female NMRI-Foxn1nu mice (6-8 weeks old, 8-10 mice per cage, engrafted subcutaneously with PC-9 HER2YVMA, NCI-H2170 HER2YVMA or NCI-N87 cells)[1]
Dosage: 10, 30 and 100 mg/kg
Administration: orally, twice daily
Result: In the NCI-H2170 HER2YVMA mechanistic model, 100 mg/kg twice daily BI-1622 resulted in a delay in tumor growth (73% TGI). In the ST3107 HER2 exon 20 mutant model, both BI-4142 (100 mg/kg twice daily) resulted in tumor regressions.
Animal Model: NMRI Foxn1nu mice (n=3 per group)[1]
Dosage: 1 mg/kg (IV); 10 and 100 mg/kg (Orally)
Administration: IV, Orally; once (Pharmacokinetic Analysis)
Result: Showed moderate in vivo clearance (50% hepatic blood flow), a moderate volume of distribution, and good to moderate bioavailability of up to 68%.
分子量

508.53

Formula

C26H24N10O2
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 (196.65 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 1.9665 mL 9.8323 mL 19.6645 mL
5 mM 0.3933 mL 1.9665 mL 3.9329 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
参考文献

BI-1622 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 1.9665 mL 9.8323 mL 19.6645 mL 49.1613 mL
5 mM 0.3933 mL 1.9665 mL 3.9329 mL 9.8323 mL
10 mM 0.1966 mL 0.9832 mL 1.9665 mL 4.9161 mL
15 mM 0.1311 mL 0.6555 mL 1.3110 mL 3.2774 mL
20 mM 0.0983 mL 0.4916 mL 0.9832 mL 2.4581 mL
25 mM 0.0787 mL 0.3933 mL 0.7866 mL 1.9665 mL
30 mM 0.0655 mL 0.3277 mL 0.6555 mL 1.6387 mL
40 mM 0.0492 mL 0.2458 mL 0.4916 mL 1.2290 mL
50 mM 0.0393 mL 0.1966 mL 0.3933 mL 0.9832 mL
60 mM 0.0328 mL 0.1639 mL 0.3277 mL 0.8194 mL
80 mM 0.0246 mL 0.1229 mL 0.2458 mL 0.6145 mL
100 mM 0.0197 mL 0.0983 mL 0.1966 mL 0.4916 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-16222681392-19-6BI1622BI 1622EGFRItkPI4KBtkCDKRafJAKEpidermal growth factor receptorErbB-1HER1Interleukin-2 inducible T-cell kinaseIL2 inducible T-cell kinasePhosphatidylinositol 4 kinasesPI4 kinasesBruton tyrosine kinaseCyclin dependent kinaseRaf kinasesJanus kinaseBa/F3 cellsNCI-H1781 cellsHEK 293 cellsH2170PC9 cellsorally activeantitumorInhibitorinhibitorinhibit

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