TGFβRI-IN-4
TGFβRI-IN-4 is a highly potent and orally active TGFβ receptor type I (TGFβRI) inhibitor, with IC50s of 44 nM and 42.5 nM for ALK5 and NIH3T3. TGFβRI-IN-4 can suppress tumor growth and tumor weight in tumor xenograft model.
For research use only. We do not sell to patients.
- CAS No.: 2421135-03-5
- Formula: C23H25F2N5O2
- Molecular Weight:441.47
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
IC50: 44 nM (ALK5), 42.5 nM (NIH3T3)[1]
TGFβRI-IN-4 (1 mg/kg and 10 mg/kg; IV and PO; single) exhibits good oral plasma exposure and excellent bioavailability[1].
Pharmacokinetic Parameters of TGFβRI-IN-4 in male Sprague-Dawley rats[1].
| IV (1 mg/kg) | PO (10 mg/kg) | |
| T1/2 (h) | 0.5 | 1.8 |
| CL (L/h/kg) | 4.9 | |
| Cmax (ng/mL) | 926.0 | |
| VSS (L/kg) | 3.0 | |
| AUC0-24 (ng/mL·h) | 195.2 | 2351.2 |
| F (%) | 120.5% |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/C mice (5-8 weeks; injected with CT26 cells)[1]
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Dosage:60 mg/kg
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Administration:PO; BID, for 21 days
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Result:Efficiently suppressed tumor growth (tumor growth inhibition = 65.7%) and tumor weight.
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Animal Model:Male BALB/C mice[1]
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Dosage:1 mg/kg and 10 mg/kg
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Administration:IV and PO; single (Pharmacokinetic Analysis)
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Result:Exhibited good oral plasma exposure and excellent bioavailability with AUC >2000 h·ng/mL and F > 80%, respectively.
Chemical Information
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CAS No. 2421135-03-5
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Molecular Weight 441.47
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Formula C23H25F2N5O2
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SMILES
CC(O)(C1=CC(NC2=CC(OC3=CN(N=C3C4CC(F)(C4)F)C5CC5)=CC=N2)=CC=N1)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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