| Identification | Back Directory | [Name]
PF-06952229 | [CAS]
1801333-55-0 | [Synonyms]
PF-06952229
3-Pyridinecarboxamide, 4-[[2-(5-chloro-2-fluorophenyl)-5-(1-methylethyl)-4-pyridinyl]amino]-N-[2-hydroxy-1-(hydroxymethyl)ethyl]- | [Molecular Formula]
C23H24ClFN4O3 | [MDL Number]
MFCD32708531 | [MOL File]
1801333-55-0.mol | [Molecular Weight]
458.91 |
| Chemical Properties | Back Directory | [Boiling point ]
704.8±60.0 °C(Predicted) | [density ]
1.341±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
12.89±0.46(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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]. | [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.
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| [References]
[1] Flavia Mercer Pernasetti, et al. Combinations of tgfb inhibitors and cdk inhibitors for the treatment of breast cancer. Patent WO2020058820A1. |
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