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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.58%
- No. CAS: 2141955-96-4
- Fòrmula: C31H42N6O4
- Peso molecular:562.70
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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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 |
Chemical Information
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No. CAS 2141955-96-4
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Appearance Solid
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Peso molecular 562.70
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Fòrmula 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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Synonyms
BLU-782; IPN-60130; ALK2-IN-1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (276 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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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. 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 Related Classifications
HY-117887 Related Classifications
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