PF-06952229


Catalog No. size PriceQuantity
M6894-2 2mg solid $242
M6894-10 10mg solid $956

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:

  1. 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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