BI-1622|cas:2681392-19-6|西域试剂

BI-1622,98.97%

产品编号：Bellancom-150023| CAS NO：2681392-19-6| 分子式：C₂₆H₂₄N₁₀O₂| 分子量：508.53

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货号	价格	库存与货期
Bellancom-150023	￥4000.00	杭州北京（现货）
Bellancom-150023	￥6800.00	杭州北京（现货）
Bellancom-150023	￥13500.00	杭州北京（现货）

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BI-1622

产品介绍

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。

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.

体外研究

BI-1622 (0-5 µM, 72 h or 96 h) inhibits the proliferation of HER2-dependent cell lines.
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.
BI-1622 displays good permeability and no PgP-mediated efflux liability.
BI-1622 shows good in vitro clearance in mouse liver microsomes and mouse hepatocytes.

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

Cell Proliferation Assay

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.
BI-1622 (0-100 mg/kg, orally, twice daily) inhibits tumor growth and inhibits oncogenic signaling in vivo.

西域 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)
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)
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%.

体内研究

西域 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)
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)
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%.

体内研究

西域 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)
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)
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%.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (196.65 mM; Need ultrasonic)

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
10 mM	0.1966 mL	0.9832 mL	1.9665 mL

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。

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)

参考文献