PD-173955
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.
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Chemical Information
| Name | PD-173955 |
|---|---|
| Iupac Chemical Name | 6-(2,6-dichlorophenyl)-8-methyl-2-((3-(methylthio)phenyl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one |
| Synonyms | PD173955; PD 173955; PD173955. |
| Molecular Formula | C21H16Cl2N4OS |
| Molecular Weight | 443.35 |
| Smile | O=C1C(C2=C(Cl)C=CC=C2Cl)=CC3=CN=C(NC4=CC=CC(SC)=C4)N=C3N1C |
| InChiKey | VAARYSWULJUGST-UHFFFAOYSA-N |
| InChi | 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) |
| CAS Number | 260415-63-2 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Solid powder |
|---|---|
| Purity | 98% Min. |
| Storage | 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 |
| Handling | |
| 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. |
| HS Code |
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| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
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3: Crespo A, Fernández A. Induced disorder in protein-ligand complexes as 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. 2008 Jul-Aug;5(4):680. Mol Pharm. 2010 Feb 1;7(1):306. Mol Pharm. 2010 Oct 4;7(5):1877. PubMed PMID: 18278867.
4: Gunby RH, Ahmed S, Sottocornola R, Gasser M, Redaelli S, Mologni L, Tartari CJ, Belloni V, Gambacorti-Passerini C, Scapozza L. Structural insights into the ATP binding pocket of the anaplastic lymphoma kinase by site-directed mutagenesis, inhibitor binding analysis, and homology modeling. J Med Chem. 2006 Sep 21;49(19):5759-68. PubMed PMID: 16970400.
5: Caligiuri M, Molz L, Liu Q, Kaplan F, Xu JP, Majeti JZ, Ramos-Kelsey R, Murthi K, Lievens S, Tavernier J, Kley N. MASPIT: three-hybrid trap for quantitative proteome fingerprinting of small molecule-protein interactions in mammalian cells. Chem Biol. 2006 Jul;13(7):711-22. PubMed PMID: 16873019.
6: Verkhivker GM. Imprint of evolutionary conservation and protein structure variation on the binding function of protein tyrosine kinases. Bioinformatics. 2006 Aug 1;22(15):1846-54. Epub 2006 May 23. PubMed PMID: 16720585.
7: Liu L, D'Mello SR. Phosphorylation of IkappaB-beta is necessary for neuronal survival. J Biol Chem. 2006 Jan 20;281(3):1506-15. Epub 2005 Nov 11. PubMed PMID: 16286457.
8: O'Hare T, Pollock R, Stoffregen EP, Keats JA, Abdullah OM, Moseson EM, 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 by AP23464, a potent ATP-based oncogenic protein kinase inhibitor: implications for CML. Blood. 2004 Oct 15;104(8):2532-9. Epub 2004 Jul 15. 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 in chronic myelogenous leukemia: molecular basis of the underlying mechanisms 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, Silver RT, Clarkson B. Direct evidence that Bcr-Abl tyrosine kinase activity disrupts normal synergistic interactions between Kit ligand and cytokines in primary primitive progenitor cells. Mol Cancer Res. 2003 Jan;1(3):176-85. PubMed PMID: 12556557.
Chemical Structure
