2421135-03-5
2421135-03-5 structure
- Name: TGFβRI-IN-4
- Chemical Name: TGFβRI-IN-4
- CAS Number: 2421135-03-5
- Molecular Formula: C23H25F2N5O2
- Molecular Weight: 441.47
- Catalog: Research Areas Cancer
- Create Date: 2022-07-02 16:08:01
- Modify Date: 2024-04-09 17:30:57
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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[1].
| Name | TGFβRI-IN-4 |
|---|
| Description | 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[1]. |
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| Related Catalog | |
| Target |
IC50: 44 nM (ALK5), 42.5 nM (NIH3T3)[1] |
| In Vivo | TGFβRI-IN-4 (compound 15r) (60 mg/kg; PO; BID, for 21 days) efficiently suppresses tumor growth and tumor weight in tumor xenograft model[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% Animal Model: Female BALB/C mice (5-8 weeks; injected with CT26 cells)[1] Dosage: 60 mg/kg Administration: PO; BID, for 21 days Result: Efficiently suppressed tumor growth (tumor growth inhibition = 65.7%) and tumor weight. Animal Model: Male BALB/C mice[1] Dosage: 1 mg/kg and 10 mg/kg Administration: IV and PO; single (Pharmacokinetic Analysis) Result: Exhibited good oral plasma exposure and excellent bioavailability with AUC >2000 h·ng/mL and F > 80%, respectively. |
| References |
| Molecular Formula | C23H25F2N5O2 |
|---|---|
| Molecular Weight | 441.47 |