PHA 665752A Met inhibitor which prevents tumorigenicity in lung cancer xenografts

PHA 665752 (CAS 477575-56-7)

PHA 665752 | CAS 477575-56-7 is rated 5.0 out of 5 by 1.
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Application: A Met inhibitor which prevents tumorigenicity in lung cancer xenografts
CAS Number: 477575-56-7
Purity: ≥98%
Molecular Weight: 641.6
Molecular Formula: C32H34Cl2N4O4S
* Refer to Certificate of Analysis for lot specific data (including water content).
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PHA 665752 is a cell-permeable pyrrolo-indolinone compound that acts as an ATP-competitive and highly potent inhibitor of Met tyrosine kinase activity (IC50 values are 9, 68, 200, 1400, 3000, 3800 and 6000 nM for Met, Ron, Flk-1, c-abl, FGFR1, EGFR and c-src respectively, and > 10000 nM for IGF-IR, PDGFR, AURORA2, PKA, PKBα, p38α, MK2 and MK3). It displays good selectivity in both cell-free kinase assays (7.5-, 22-, 155-, and ≥333-fold over Ron, Flk1, c-abl, and a panel of 12 other commonly studied kinases, respectively) and in receptor autophosphorylation in cells (20- and 60-fold over Ron and Flk1, respectively). PHA 665752 is shown to suppress Met-mediated cellular functions in vitro and inhibit tumorigenicity and angiogenesis in mouse lung cancer xenografts.


References

1. Christensen, J.G., et al. 2003. Cancer Res. 63: 7345-7355. PMID: 14612533
2. Smolen, G.A., et al. 2006. Proc. Natl. Acad. Sci. U.S.A. 103: 2316-2321. PMID: 16461907
3. Puri, N., et al. 2007. Cancer Res. 67: 3529-3534. PMID: 17440059
4. Yang, Y., et al. 2008. Mol. Cancer Ther. 7: 952-960. PMID: 18413809

Physical State :
Solid
Solubility :
Soluble in DMSO (100 mM).
Storage :
Store at 4° C
Boiling Point :
~890.17° C at 760 mmHg (Predicted)
Density :
~1.40 g/cm3 (Predicted)
Refractive Index :
n20D 1.66 (Predicted)
Optical Activity :
α20/D +60°±10°, c = 0.2 in methanol; α20/D +47°, c = 1 in methanol
IC50 :
Met: IC50 = 9 nM; Ron: IC50 = 68 nM; Flk-1: IC50 = 0.2 µM; c-Abl: IC50 = 1.4 µM; Flg: IC50 = 3 µM
pK Values :
pKa: 11.39 (Predicted), pKb: 9.13 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
10461815
MDL Number :
MFCD07772270
SMILES :
O=C1Nc2ccc(cc2/C/1=C/c1[nH]c(C)c(C(=O)N2CCC[C@@H]2CN2CCCC2)c1C)S(=O)(=O)Cc1c(Cl)cccc1Cl

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Certificate of Analysis

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PHA 665752  Product Citations

See how others have used PHA 665752. Click on the entry to view the PubMed entry .

Citations 1 to 10 of 15 total

PMID: # 28429746  Miura, Y.|Ngo Thai Bich, V.|Furuya, M.|Hasegawa, H.|Takahashi, S.|Katagiri, N.|Hongu, T.|Funakoshi, Y.|Ohbayashi, N.|Kanaho, Y.| et al. 2017. Sci Rep. 7: 46649.

PMID: # 26875548  Yoon, YS. et al. 2016. Sci Rep. 6: 20992.

PMID: # 25934697  Walsh, AM. et al. 2015. Mol. Cancer Res. 13: 1227-37.

PMID: # 25986930  Lan, YW. et al. 2015. Stem Cell Res Ther. 6: 97.

PMID: # 26351321  Sugano, T. et al. 2015. Mol. Cancer Ther. 14: 2433-40.

PMID: # 24959005  Byun, JY. et al. 2014. Mediators Inflamm. 2014: 463524.

PMID: # 24673557  Aenlle, KK. et al. 2014. Mol. Endocrinol. 28: 722-30.

PMID: # 24951116  Furcht, C.M. et al. 2014. Journal of cell science. 127: 3555-67.

PMID: # 23584089  Sadanandam, A. et al. 2013. Nat. Med. 19: 619-25.

PMID: # 22902361  Fialin, C. et al. 2013. Leukemia. 27: 325-35.

Citations 1 to 10 of 15 total
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Rated 5 out of 5 by from Tsai Tsai, et al. (PubMed ID 26277884) found that PHA665752, a c-Met specific inhibitor, mitigated ERK1/2 and Akt phosphorylation, cell migration/invasion. It also dissipated changes in expression of EMT markers that have been induced by HGF. -SCBT Publication Review
Date published: 2015-06-27
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