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PD173955

PD173955 Struktur
260415-63-2
CAS-Nr.
260415-63-2
Englisch Name:
PD173955
Synonyma:
CS-1508;PD-173955;CHEBI:49791;PD173955 USP/EP/BP;PD173955, 10 mM in DMSO;PD173955; CHEBI:49791; 260415-63-2; PD-173955;6-(2,6-dichlorophenyl)-8-methyl-2-(3-methylsulfanylanilino)pyrido[2,3-d]pyrimidin-7-one;6-(2,6-Dichlorophenyl)-8-methyl-2-((3-(methylthio)phenyl)amino)pyrido[2,3-d]pyrimidin-7(8H)-on;6-(2,6-Dichlorophenyl)-8-methyl-2-[[3-(methylthio)phenyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one;Pyrido[2,3-d]pyrimidin-7(8H)-one, 6-(2,6-dichlorophenyl)-8-methyl-2-[[3-(methylthio)phenyl]amino]-
CBNumber:
CB82485076
Summenformel:
C21H16Cl2N4OS
Molgewicht:
443.35
MOL-Datei:
260415-63-2.mol

PD173955 Eigenschaften

Dichte
1.49
storage temp. 
Store at -20° C
L?slichkeit
≥22.15 mg/mL in DMSO with gentle warming
Aggregatzustand
White powder.
Farbe
White to yellow
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)
InChIKey
VAARYSWULJUGST-UHFFFAOYSA-N
SMILES
S(C)c1cc(ccc1)Nc2nc3c(cn2)C=C(C(=O)N3C)c4c(cccc4Cl)Cl

Sicherheit

WGK Germany  WGK 3
Speicherklasse 11 - Combustible Solids

PD173955 Chemische Eigenschaften,Einsatz,Produktion Methoden

Enzyminhibitor

This tyrosine kinase inhibitor (FW = 443.35 g/mol; CAS 260415-63-2; Solubility: <1 mg/mL DMSO, Ethanol, H2O), 6-(2,6-dichlorophenyl)-8- methyl-2-((3-(methylthio)phenyl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one targets Bcr-Abl (IC50 = 1-2 nM, in vitro), the constitutively active tyrosine kinase that results from inadvertent fusion of bcr and abl genes and that causes oncogenic transformation in chronic myelogenous leukemia, or CML, inhibiting Bcr-Abl-dependent cell growth with an IC50 of 2-35 nM in different cell lines. PD173955 also inhibits kit ligand-dependent c-kit autophosphorylation (IC50 = ~25 nM) and kit ligand-dependent proliferation of M07e cells (IC50 = 40 nM), but had a lesser effect on interleukin 3- dependent (IC50 = 250 nM) or granulocyte macrophage colony-stimulating factor (IC50 = 1 μM)-dependent cell growth. PD173955 also increases the susceptibility of HT29 cells to detachment-induced apoptosis (anoikis) in a dose- and time-dependent manner. Structural Features Distinguishing Imatinib & PD173955 Binding: Crystal structures of Abl kinase domain complexes with imatinib (Gleevec) and PD173955 show that both bind to the canonical ATP-binding site, but in distinctive ways. Imatinib captures a specific inactive conformation of Abl’s activation loop, mimicking the bound peptide substrate. In contrast, PD173955 binds to the Abl activation loop in a way that resembles the active kinase conformation. The 10x greater potency of PD173955 over imatinib is attributed to its ability to target multiple active and inactive forms of Abl, whereas imatinib binds only to a specific catalytically inactive conformation (4

PD173955 Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


PD173955 Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Global( 122)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
Capot Chemical Co.,Ltd.
+86-(0)57185586718 +86-13336195806
sales@capot.com China 29640 60
ATK CHEMICAL COMPANY LIMITED
+undefined-21-51877795
ivan@atkchemical.com China 33024 60
CONIER CHEM AND PHARMA LIMITED
+8618523575427
sales@conier.com China 49979 58
TargetMol Chemicals Inc.
+1-781-999-5354; +17819995354
marketing@targetmol.com United States 32466 58
Dideu Industries Group Limited
+86-29-89586680 +86-15129568250
1026@dideu.com China 28509 58
BOC Sciences
16314854226; +16314854226
inquiry@bocsci.com United States 19853 58
Hefei Hirisun Pharmatech Co., Ltd
+8615056975894
shawn@hirisunpharm.com CHINA 9911 58
InvivoChem
+1-708-310-1919 +1-13798911105
sales@invivochem.cn United States 6391 58
HANGZHOU LEAP CHEM CO., LTD.
+86-571-87711850
market18@leapchem.com China 24597 58
TargetMol Chemicals Inc.
+1-781-999-5354;
support@targetmol.com United States 39040 58

260415-63-2()Verwandte Suche:


  • PD-173955
  • 6-(2,6-Dichlorophenyl)-8-methyl-2-[[3-(methylthio)phenyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one PD-173955
  • 6-(2,6-Dichlorophenyl)-8-methyl-2-[[3-(methylthio)phenyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one
  • 6-(2,6-dichlorophenyl)-8-methyl-2-(3-methylsulfanylanilino)pyrido[2,3-d]pyrimidin-7-one
  • 6-(2,6-Dichlorophenyl)-8-methyl-2-((3-(methylthio)phenyl)amino)pyrido[2,3-d]pyrimidin-7(8H)-on
  • CHEBI:49791
  • PD173955; CHEBI:49791; 260415-63-2; PD-173955
  • CS-1508
  • Pyrido[2,3-d]pyrimidin-7(8H)-one, 6-(2,6-dichlorophenyl)-8-methyl-2-[[3-(methylthio)phenyl]amino]-
  • PD173955 USP/EP/BP
  • PD173955, 10 mM in DMSO
  • 260415-63-2
  • Inhibitors
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