BI-4732
Based on 1 Customer Validation
BI-4732 is an orally active, reversible, ATP-competitive EGFR inhibitor with blood-brain barrier penetration. BI-4732 inhibits the kinase activity of EGFR L858R, T790M and C797S with IC50 values of 1 nM while sparing EGFR wild-type. BI-4732 inhibits EGFR and reduces the phosphorylation of AKT, ERK, and S6K. BI-4732 demonstrates excellent intracranial anti-tumor efficacy in YU-1097 xenograft model harboring EGFR_E19del/T790M/C797S. BI-4732 can be used for the study of non-small cell lung cancer (NSCLC).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.81%
- CAS 番号: 2769715-68-4
- 分子式: C32H36N10O2
- 分子量:592.69
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保管条件:
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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
EGFR アイソフォーム固有の製品をすべて表示
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生物活性
BI-4732(1-1000 nM, 72 h) exhibits potent anti-proliferative activity against EGFR_E19del/C797S (IC50 = 6 nM), EGFR_L858R/C797S (IC50 = 213 nM), EGFR_E19del/T790M/C797S (IC50 = 4 nM), and EGFR_L858R/T790M/C797S (IC50 = 15 nM) in Ba/F3 cells[1].
BI-4732(10-100 nM, 6 h) inhibits EGFR and downstream signaling phosphorylation in all EGFR_C797S Ba/F3 cells when combined with Osimertinib (HY-15772)[1].
BI-4732 (1-1000 nM, 72 h) shows potent antiproliferative activity against YU-1182, YU-1097, YUO-143, PC9, and PC9_DC cells, with [1].
values of 73 nM, 3 nM, 5 nM, 14 nM, and 25 nM, respectively[1].
BI-4732 (1-30 nM, 21 days) almost completely prevents clonogenicity in YUX-1024, PC9_DC, YU-1182 and YU-1097 cells when combined with Osimertinib (HY-15772)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:All EGFR_C797S Ba/F3 cells
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Concentration:10, 100 nM combined with Osimertinib
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Incubation Time:6 h
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Result:Reduced the phosphorylation of AKT, ERK, and S6K.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:YU-1097 cells (5 × 106 in 100 µL PBS) were subcutaneously implanted into the flanks of 6-week-old female BALB/c nude mice[1]
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Dosage:2.5, 5, 10, 25 mg/kg or 5 mg/kg combined with Osimertinib (25 mg/kg)
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Administration:p.o. twice daily for 4 weeks
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Result:Achieved tumor growth inhibition (TGI) rates of 143.1%, 154.0%, 174.1%, and 183.2% at doses of 2.5, 5, 10, and 25 mg/kg, respectively.
Showed no significant changes in body weight.
Reduced the Ki67 expression.
Appeared phosphorylation of EGFR and its downstream molecules, AKT, ERK, and S6K after 6 h.
Showed greater tumor regression with 176.2% TGI when combined with Osimertinib.
化学情報
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CAS 番号 2769715-68-4
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性状 Solid
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分子量 592.69
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分子式 C32H36N10O2
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Color Light yellow to yellow
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SMILES
CC1=C(C=NN2C3=NC(N4C[C@@H]5OC[C@H]4C5)=C6C(N(C)C(N7C[C@@H](CCC8)N8CC7)=N6)=C3)C2=CC(C9=C(OC)C=CN=C9)=N1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶剤 & 溶解度
DMSO : 2 mg/mL (3.37 mM; ultrasonic and warming and heat to 60°C; 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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
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- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6872 mL | 8.4361 mL | 16.8722 mL | 42.1806 mL |
BI-4732 関連分類
HY-161275 関連分類
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