PF 573228
Synonym(s):6-[4-(3-Methanesulfonyl-benzylamino)-5-trifluoromethyl-pyrimidin-2-ylamino]-3,4-dihydro-1H-quinolin-2-one;Focal Adhesion Kinase Inhibitor II - CAS 869288-64-2 - Calbiochem;PF-228;PF-573,228, PF-228, 6-((4-((3-(Methanesulfonyl)benzyl)amino)-5-trifluoromethylpyrimidin-2-yl)amino)-3,4-dihydro-1H-quinolin-2-one, FAK Inhibitor II, Cdk7 Inhibitor V
- CAS NO.:869288-64-2
- Empirical Formula: C22H20F3N5O3S
- Molecular Weight: 491.49
- MDL number: MFCD11519967
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-01 18:44:47
What is PF 573228?
Description
Focal adhesion kinases (FAKs) are non-receptor tyrosine kinases that play roles in regulating diverse processes, including cell adhesion, spreading, migration, proliferation, and apoptosis. They are overexpressed in many types of cancer. PF-573228 inhibits FAK with IC50 values of 4 and 30-100 nM for a purified recombinant catalytic fragment of FAK and in cultured cells, respectively. It is 50-250-fold selective for FAK over other protein kinases. PF-573228 can inhibit chemotactic and haptotactic migration of cells as well as prevent focal adhesion turnover.
The Uses of PF 573228
A novel focal adhesion kinase inhibitor that has been shown to suppress the adverse phenotype of endocrine-resistant breast cancer cells and improve endocrine response in endocrine-sensitive cells.
Definition
ChEBI: 6-[[4-[(3-methylsulfonylphenyl)methylamino]-5-(trifluoromethyl)-2-pyrimidinyl]amino]-3,4-dihydro-1H-quinolin-2-one is a member of quinolines.
Biochem/physiol Actions
PF-573228 is a focal adhesion kinase (FAK) inhibitor; Non-receptor tyrosine kinase inhibitor.
storage
Store at +4°C
References
[1]. slack-davis, j.k., et al., cellular characterization of a novel focal adhesion kinase inhibitor. j biol chem, 2007. 282(20): p. 14845-52.
[2]. golubovskaya, v.m., focal adhesion kinase as a cancer therapy target. anticancer agents med chem, 2010. 10(10): p. 735-41.
[3]. cabrita, m.a., et al., focal adhesion kinase inhibitors are potent anti-angiogenic agents. mol oncol, 2011. 5(6): p. 517-26.
[4]. al-toub, m., et al., pleiotropic effects of cancer cells' secreted factors on human stromal (mesenchymal) stem cells. stem cell res ther, 2013. 4(5): p. 114.
[5]. so, e.c., et al., evidence for activation of bk ca channels by a known inhibitor of focal adhesion kinase, pf573228. life sci, 2011. 89(19-20): p. 691-701.
Properties of PF 573228
Melting point: | >242°C (dec.) |
Density | 1.459 |
storage temp. | 2-8°C |
solubility | DMSO: ≥20mg/mL |
form | powder |
pka | 14.30±0.20(Predicted) |
color | white to off-white |
Safety information for PF 573228
Signal word | Danger |
Pictogram(s) |
Skull and Crossbones Acute Toxicity GHS06 |
GHS Hazard Statements |
H301:Acute toxicity,oral H319:Serious eye damage/eye irritation |
Precautionary Statement Codes |
P301+P310:IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for PF 573228
InChIKey | HESLKTSGTIBHJU-UHFFFAOYSA-N |
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