1. TGF-beta/Smad
  2. TGF-β Receptor
  3. PF-06952229

PF-06952229 

Cat. No.: HY-136244
Handling Instructions

PF-06952229 is a potent, selective and orally active TGFbR1 inhibitor. PF-06952229 specifically binds to TGFbR1 and prevents TGFbR1-mediated signal transduction. PF-06952229 is a promising antineoplastic agent for the study solid tumors, especifically metastatic breast cancer.

For research use only. We do not sell to patients.

PF-06952229 Chemical Structure

PF-06952229 Chemical Structure

CAS No. : 1801333-55-0

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Description

PF-06952229 is a potent, selective and orally active TGFbR1 inhibitor. PF-06952229 specifically binds to TGFbR1 and prevents TGFbR1-mediated signal transduction. PF-06952229 is a promising antineoplastic agent for the study solid tumors, especifically metastatic breast cancer[1].

IC50 & Target

IC50: transforming growth factor-beta receptor 1 (TGFbR1)[1]

In Vivo

PF-06952229 (oral gavage; 30 mg/kg; twice daily; 21 days) combines with Palbociclib 21 days results in an improved inhibition of pSMAD2 in the MCF7 ER+ xenograft breast cancer tumor model. This combination also leads to a significant increase in survival relative to PF-06952229 monotherapy[1].

Animal Model: MCF-7 ER+ HER2-xenograft breast cancer tumor model[1]
Dosage: 30 mg/kg
Administration: Oral gavage; twice daily; 44 days
Result: Resulted in an increase in tumor growth inhibition when combined with Palbociclib.
Molecular Weight

458.91

Formula

C₂₃H₂₄ClFN₄O₃

CAS No.

1801333-55-0

SMILES

O=C(NC(CO)CO)C1=CN=CC=C1NC2=CC(C3=CC(Cl)=CC=C3F)=NC=C2C(C)C

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

PF-06952229PF06952229PF 06952229TGF-β ReceptorTransforming growth factor beta receptorsbreastcancerCT26cellsMCF-7SolidtumorsMetastaticdifferentiationapoptosismotilityinvasionangiogenesisInhibitorinhibitorinhibit

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PF-06952229
Cat. No.:
HY-136244
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