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  4. BI-1622

BI-1622 是一種口服有效的和高選擇性 HER2 (ERBB2) 抑制劑，IC50 為 7 nM。BI-1622對 EGFR 的選擇性大于 25 倍。BI-1622 在轉(zhuǎn)染 H2170 和 PC9 細(xì)胞的移植瘤小鼠模型中表現(xiàn)出較高的體內(nèi)的抗腫瘤效果，具有良好的活性分子代謝和藥代動力學(xué)特性。

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BI-1622 Chemical Structure

BI-1622 Chemical Structure

CAS No. : 2681392-19-6

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規(guī)格 價格 是否有貨 數(shù)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   詢價  
100 mg   詢價  

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Customer Review

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  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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

 

體外研究
(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.

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.
體內(nèi)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 號
性狀

固體

顏色

Light yellow to yellow

運(yùn)輸條件

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

4°C, protect from light

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

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 100 mg/mL (196.65 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)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
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲存時，請?jiān)?個月內(nèi)使用，-20°C儲存時，請?jiān)?個月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計(jì)算器
請輸入動物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實(shí)驗(yàn)過程有損耗，建議您多配一只動物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料
參考文獻(xiàn)

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲存時，請?jiān)?個月內(nèi)使用，-20°C儲存時，請?jiān)?個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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.

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產(chǎn)品名稱：
BI-1622
目錄號：
HY-150023
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