2. TGF-beta/Smad
  3. TGF-β Receptor
  4. 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.

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TGFβRI-IN-4 Chemical Structure

TGFβRI-IN-4 Chemical Structure

CAS No. : 2421135-03-5

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TGFβRI-IN-4 Related Antibodies

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ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B

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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].

IC50 & 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%

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

441.47

Formula

C23H25F2N5O2
CAS No.
SMILES

CC(O)(C1=CC(NC2=CC(OC3=CN(N=C3C4CC(F)(C4)F)C5CC5)=CC=N2)=CC=N1)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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TGFβRI-IN-4 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TGFβRI-IN-42421135-03-5TGF-β ReceptorTransforming growth factor beta receptorsAntitumorTumor xenograft modelBALB/C miceALK5NIH3T3Orally activeInhibitorinhibitorinhibit

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