BLU-654
BLU-654 is an orally active antineoplastic agent and KIT inhibitor. BLU-654 is a highly selective inhibitor targeting wild-type KIT, PDGFRβ, and KITV654A over most other kinases in the kinome. BLU-654 exerts sustained antineoplastic activity in KITV654A cell-derived xenograft mouse models. BLU-654 can be used in research related to Imatinib (HY-15463)-resistant gastrointestinal stromal tumors.
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。
- CAS 番号: 2999638-62-7
- 分子式: C21H28FN7O2
- 分子量:429.49
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
BLU-654 potently inhibits the autophosphorylation of KIT in HMC1.1 11/13 cells, with an IC50 of 5.7 nM[1].
BLU-654 inhibits the autophosphorylation of wild-type KIT in M-07e cells with an IC50 of 82.7 nM, and is 15-fold more selective for KITV654A than for wild-type KIT[1].
BLU-654 inhibits the autophosphorylation of PDGFRβ in SW569 cells with an IC50 of 1251.4 nM, and is 219-fold more selective for KITV654A than for PDGFRβ[1].
BLU-654 exhibits species-dependent metabolic stability, with no intrinsic clearance in human and canine liver microsomes, low clearance (2 mL·min-1·kg-1) in human hepatocytes, and higher clearance in rat, canine and cynomolgus monkey hepatocytes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD-SCID mice[1]
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Dosage:1-30 mg/kg (PK/PD); 3-60 mg/kg (Efficacy)
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Administration:p.o.; daily; 27 days (Efficacy); single dose (PK/PD)
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Result:Elicited a dose- and time-dependent reduction in pSTAT5, with a free in vivo IC50 of 4.2 nM at 4 hours.
Reduced pSTAT5 by 95% over 4 hours at 10 mg/kg, with levels returning to 68% of baseline at 24 hours.
Achieved dose-dependent plasma exposures, exceeding the in vitro pKIT IC50 at most doses 10 hours postdosing, and at 30 mg/kg, exposures remained above the in vitro IC50 for up to 24 hours.
Showed slower tumor growth in mice treated with 3 mg/kg compared to controls after 27 days of daily dosing.
Eliminated tumors in mice treated with 10, 30, and 60 mg/kg, with no tumor regrowth observed during the 48-day post-treatment observation period.
Maintained body weight within 10% of baseline across all doses, indicating good tolerability.
化学情報
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CAS 番号 2999638-62-7
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分子量 429.49
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分子式 C21H28FN7O2
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SMILES
F[C@@H](C)C1=NC(N)=CC(NC2=NC=C(C3=CN(CC(C)(O)C)N=C3)C(OC(C)C)=C2)=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
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
BLU-654 関連分類
HY-182043 関連分類
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