1801333-55-0

1801333-55-0 structure

Name: PF-06952229
Chemical Name: PF-06952229
CAS Number: 1801333-55-0
Molecular Formula: C₂₃H₂₄ClFN₄O₃
Molecular Weight: 458.91
Create Date: 2020-06-01 18:03:25
Modify Date: 2025-08-27 06:01:05
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].

Name	PF-06952229

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].
Related Catalog	Research Areas >> Cancer
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.
References	[1]. Flavia Mercer Pernasetti, et al. Combinations of tgfb inhibitors and cdk inhibitors for the treatment of breast cancer. Patent WO2020058820A1.

Molecular Formula	C₂₃H₂₄ClFN₄O₃
Molecular Weight	458.91