PD-173955

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WARNING: This product is for research use only, not for human or veterinary use.

Description:PD-173955 is a src tyrosine kinase inhibitor. PD173955 inhibited Bcr-Abl-dependent cell growth. PD173955 showed cell cycle arrest in G(1). PD173955 has an IC(50) of 1-2 nM in kinase inhibition assays of Bcr-Abl, and in cellular growth assays it inhibits Bcr-Abl-dependent substrate tyrosine phosphorylation. PD173955 inhibited kit ligand-dependent c-kit autophosphorylation (IC(50) = approximately 25 nM) and kit ligand-dependent proliferation of M07e cells (IC(50) = 40 nM) but had a lesser effect on interleukin 3-dependent (IC(50) = 250 nM) or granulocyte macrophage colony-stimulating factor (IC(50) = 1 microM)-dependent cell growth.

Price and Availability

PD173955, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.

Chemical Structure

Theoretical Analysis

MedKoo Cat#: 406164Name: PD-173955CAS#: 260415-63-2Chemical Formula: C21H16Cl2N4OSExact Mass: 442.04219Molecular Weight: 443.34894Elemental Analysis: C, 56.89; H, 3.64; Cl, 15.99; N, 12.64; O, 3.61; S, 7.23

Synonym:PD173955; PD 173955; PD173955.

IUPAC/Chemical Name:6-(2,6-dichlorophenyl)-8-methyl-2-((3-(methylthio)phenyl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one

InChi Key:VAARYSWULJUGST-UHFFFAOYSA-N

InChi Code:InChI=1S/C21H16Cl2N4OS/c1-27-19-12(9-15(20(27)28)18-16(22)7-4-8-17(18)23)11-24-21(26-19)25-13-5-3-6-14(10-13)29-2/h3-11H,1-2H3,(H,24,25,26)

SMILES Code:O=C1C(C2=C(Cl)C=CC=C2Cl)=CC3=CN=C(NC4=CC=CC(SC)=C4)N=C3N1C

Technical Data

Additional Information

References

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3: Crespo A, Fernández A. Induced disorder in protein-ligand complexesas a drug-design strategy. Mol Pharm. 2008 May-Jun;5(3):430-7. doi:10.1021/mp700148h. Epub 2008 Feb 16. Erratum in: Mol Pharm. 2008Jul-Aug;5(4):680. Mol Pharm. 2010 Feb 1;7(1):306. Mol Pharm. 2010 Oct4;7(5):1877. PubMed PMID: 18278867.

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6: Verkhivker GM. Imprint of evolutionary conservation and proteinstructure variation on the binding function of protein tyrosine kinases.Bioinformatics. 2006 Aug 1;22(15):1846-54. Epub 2006 May 23. PubMedPMID: 16720585.

7: Liu L, D"Mello SR. Phosphorylation of IkappaB-beta is necessary forneuronal survival. J Biol Chem. 2006 Jan 20;281(3):1506-15. Epub 2005Nov 11. PubMed PMID: 16286457.

8: O"Hare T, Pollock R, Stoffregen EP, Keats JA, Abdullah OM, MosesonEM, Rivera VM, Tang H, Metcalf CA 3rd, Bohacek RS, Wang Y,Sundaramoorthi R, Shakespeare WC, Dalgarno D, Clackson T, Sawyer TK,Deininger MW, Druker BJ. Inhibition of wild-type and mutant Bcr-Abl byAP23464, a potent ATP-based oncogenic protein kinase inhibitor:implications for CML. Blood. 2004 Oct 15;104(8):2532-9. Epub 2004 Jul15. PubMed PMID: 15256422.

9: Cowan-Jacob SW, Guez V, Fendrich G, Griffin JD, Fabbro D, Furet P,Liebetanz J, Mestan J, Manley PW. Imatinib (STI571) resistance inchronic myelogenous leukemia: molecular basis of the underlyingmechanisms and potential strategies for treatment. Mini Rev Med Chem.2004 Mar;4(3):285-99. Review. PubMed PMID: 15032675.

10: Strife A, Wisniewski D, Liu C, Lambek CL, Darzynkiewicz Z, SilverRT, Clarkson B. Direct evidence that Bcr-Abl tyrosine kinase activitydisrupts normal synergistic interactions between Kit ligand andcytokines in primary primitive progenitor cells. Mol Cancer Res. 2003Jan;1(3):176-85. PubMed PMID: 12556557.