BI-1622
Based on 1 Customer Validation
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.
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- Pureza : 98.02%
- No. CAS: 2681392-19-6
- Fòrmula: C26H24N10O2
- Peso molecular:508.53
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
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HER2 7 nM (IC50) |
ErbB4 |
EGFR |
CDK11B |
JAK3 |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Ba/F3 cells
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Concentration:0-5 µM
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Incubation Time:72 h or 96 h
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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.
In Vivo
BI-1622 (0-100 mg/kg, orally, twice daily) inhibits tumor growth and inhibits oncogenic signaling in vivo[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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]
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Dosage:10, 30 and 100 mg/kg
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Administration:orally, twice daily
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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.
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Animal Model:NMRI Foxn1nu mice (n=3 per group)[1]
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Dosage:1 mg/kg (IV); 10 and 100 mg/kg (Orally)
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Administration:IV, Orally; once (Pharmacokinetic Analysis)
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Result:Showed moderate in vivo clearance (50% hepatic blood flow), a moderate volume of distribution, and good to moderate bioavailability of up to 68%.
Chemical Information
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No. CAS 2681392-19-6
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Appearance Solid
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Peso molecular 508.53
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Fòrmula C26H24N10O2
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Color Light yellow to yellow
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SMILES
O=C(N1CCN(CC1)C2=NC3=C(NC4=CC=C(C(C)=C4)OC5=CC6=NC=NN6C=C5)N=CN=C3C=N2)C=C
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (196.65 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| 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 |
BI-1622 Related Classifications
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