PF-06952229


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

Description

Cas:1801333-55-0

Product Information

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.

 

Chemical Formula: C23H24ClFN4O3

 

Exact Mass: 458.1521

 

Molecular Weight: 458.9184

 

Elemental Analysis: C, 60.20; H, 5.27; Cl, 7.72; F, 4.14; N, 12.21; O, 10.46

 

Chemical Name: 4-((2-(5-chloro-2-fluorophenyl)-5-isopropylpyridin-4-yl)amino)-N-(1,3-dihydroxypropan-2-yl)nicotinamide

 

InChi Key: 

IPBLCOKXDQHSQW-UHFFFAOYSA-N

 

InChi Code: 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)

 

Smiles Code:

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

 

 

Technical Data:

 

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

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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