BMS-906024
Based on 3 publication(s) in Google Scholar
BMS-906024 is an orally active and selective γ-secretase (gamma secretase) inhibitor. BMS-906024 is a potent pan-Notch receptors inhibitor with IC50s of 1.6 nM, 0.7 nM, 3.4 nM, and 2.9 nM for Notch1, -2, -3, and -4 receptors, respectively. BMS-906024 demonstrates broad-spectrum antineoplastic activity.
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- 純度: 99.91%
- CAS 番号: 1401066-79-2
- 分子式: C26H26F6N4O3
- 分子量:556.50
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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
MedChemExpress（MCE）の使用を引用している文献 BMS-906024
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生物活性
IC50: 1.6 nM (Notch1), 0.7 nM (Notch2), 3.4 nM (Notch3) and 2.9 nM (Notch4)[2]
BMS-906024 (5-100 nM; 72 hours) reduces Notch1 ICD levels in all six lung cancer cell lines. BMS-906024 at 100 nM, has no effect on total Notch1, and down-regulated Hes1 transcript[1].
In cancer cell proliferation assays, BMS-906024 inhibits both leukemia (TALL-1) and triple-negative breast cancer (MDA-MB-468) cells with IC50 of ～4 nM[2].
BMS-906024 (100 nM; for 72 hours) enhances the anti-tumor activity of Paclitaxel in vitro[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NSCLC cell lines (A549, H358, H1975, H2444, H1792, HCC44)
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Concentration:5, 10, 25, 50, 100 nM
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Incubation Time:72 hours
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Result:Reduced Notch1 ICD levels in all six lung cancer cell lines tested at concentrations as low as 5 nM, with maximal depletion at 50-100 nM.
BMS-906024 has a T1/2 of 4.6/5.3 hours, a Cmax of 1/0.3 μM and an AUC of 3.4/1.9 μM hour for IV/PO[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Six to 12-week-old female NOD scid gamma (NSG) mice with KRAS- and BRAF-WT PDX-T42 xenografts[1]
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Dosage:8.5 mg/kg
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Administration:oral gavage; days 1 through 4 of each week for 3 weeks
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Result:Significantly enhanced the tumor growth inhibition of Paclitaxel (36 mg/kg), but had no significant effect on Cisplatin (2 mg/kg) treatment.
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Animal Model:Mouse[2]
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Dosage:1 mg/kg (Pharmacokinetic Analysis)
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Administration:IV or PO
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Result:Had a T1/2 of 4.6/5.3 hours, a Cmax of 1/0.3 μM and an AUC of 3.4/1.9 μM•hour for IV/PO.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1401066-79-2
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性状 Solid
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分子量 556.50
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分子式 C26H26F6N4O3
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Color White to off-white
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SMILES
O=C(N[C@@H]1C(N(C)C2=CC=CC=C2C(C3=CC=CC=C3)=N1)=O)[C@H](CCC(F)(F)F)[C@H](CCC(F)(F)F)C(N)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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bioRxiv
Design of combination therapeutics from protein response to drugs in ovarian cancer cells. [Abstract]2025 May 2:2025.04.28.651139. PMID: 40568132 -
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溶剤 & 溶解度
DMSO : 9.5 mg/mL (17.07 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. 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. 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 (286 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Morgan KM, et al. Gamma Secretase Inhibition by BMS-906024 Enhances Efficacy of Paclitaxel in Lung Adenocarcinoma. Mol Cancer Ther. 2017 Dec;16(12):2759-2769. [Content Brief]
[2]. Gavai AV, et al. Discovery of Clinical Candidate BMS-906024: A Potent Pan-Notch Inhibitor for the Treatment of Leukemia and Solid Tumors. ACS Med Chem Lett. 2015 Mar 11;6(5):523-7. [Content Brief]
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. 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 | 1.7969 mL | 8.9847 mL | 17.9695 mL | 44.9236 mL |
| 5 mM | 0.3594 mL | 1.7969 mL | 3.5939 mL | 8.9847 mL | |
| 10 mM | 0.1797 mL | 0.8985 mL | 1.7969 mL | 4.4924 mL | |
| 15 mM | 0.1198 mL | 0.5990 mL | 1.1980 mL | 2.9949 mL |
BMS-906024 関連分類
HY-15670 関連分類
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