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.
Product information
CAS Number: 1801333-55-0
Molecular Weight: 458.91
Formula: C23H24ClFN4O3
Chemical Name: 4-((2-(5-chloro-2-fluorophenyl)-5-isopropylpyridin-4-yl)amino)-N-(1,3-dihydroxypropan-2-yl)nicotinamide
Smiles: CC(C)C1=CN=C(C=C1NC1=CC=NC=C1C(=O)NC(CO)CO)C1=CC(Cl)=CC=C1F
InChiKey: IPBLCOKXDQHSQW-UHFFFAOYSA-N
InChi: InChI=1S/C23H24ClFN4O3/c1-13(2)17-10-27-21(16-7-14(24)3-4-19(16)25)8-22(17)29-20-5-6-26-9-18(20)23(32)28-15(11-30)12-31/h3-10,13,15,30-31H,11-12H2,1-2H3,(H,28,32)(H,26,27,29)
Technical Data
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
In Vitro:
IC50: transforming growth factor-beta receptor 1 (TGFbR1).
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.
References:
- Flavia Mercer Pernasetti, et al. Combinations of tgfb inhibitors and cdk inhibitors for the treatment of breast cancer. Patent WO2020058820A1.
Products are for research use only. Not for human use.
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