Fidrisertib
Based on 1 Customer Validation
Fidrisertib (BLU-782) is the orally active inhibitor for activin receptor-like kinase 2 (ALK2) that inhibits ALK2R206H, ALK2, ALK1, ALK6, ALK3, ALK4, TGFβR2 and ALK5 with IC50s of 0.2, 0.6, 3, 24, 45, 65, 67 and 155 nM, respectively.
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: 98.58%
- CAS 番号: 2141955-96-4
- 分子式: C31H42N6O4
- 分子量:562.70
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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
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生物活性
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ALK2 R206H 0.2 nM (IC50) |
ALK2 0.6 nM (IC50) |
ALK1 3 nM (IC50) |
ALK6 24 nM (IC50) |
ALK4 65 nM (IC50) |
TGF-βR2 67 nM (IC50) |
ALK5 155 nM (IC50) |
ACVR2A 9096 nM (IC50) |
Fidrisertib inhibits the activity of ALK2R206H in cell HEK293T/ALK3KO with an IC50 of 7 nM[2].
Fidrisertib blocks the signaling pathway activated by ligands such as BMP and activin, reduces the phosphorylation of SMAD1, thereby inhibiting the heterotopic ossification[2].
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:ALK2R206H knock-in mouse model[2]
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Dosage:50 mg/kg
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Administration:po or ip, once daily for 3-7 days
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Result:Prevented heterotopic ossification after muscle injury (pinch injury) and fracture (fibular osteotomy).
Exhibited normal muscle repair response after muscle injury and normal healing after fracture.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2141955-96-4
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性状 Solid
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分子量 562.70
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分子式 C31H42N6O4
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Color Yellow to brown
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SMILES
O=C(N1CCN(C2=CC=NN3C2=CC(C4=NC=C(C5(OCC)CCN(C(C)C)CC5)C=C4)=C3)CC1)O[C@H]6COCC6
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別名
BLU-782; IPN-60130; ALK2-IN-1
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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
溶剤 & 溶解度
DMSO : 4.17 mg/mL (7.41 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 (276 KB)
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SDS (393 KB)
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- 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
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 | 1.7771 mL | 8.8857 mL | 17.7715 mL | 44.4286 mL |
| 5 mM | 0.3554 mL | 1.7771 mL | 3.5543 mL | 8.8857 mL |
Fidrisertib 関連分類
HY-117887 関連分類
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