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; 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]-;6-(2,6-Dichlorophenyl)-8-methyl-2-[[3-(methylthio)phenyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one PD-173955
CBNumber:
CB82485076
Summenformel:
C21H16Cl2N4OS
Molgewicht:
443.35
MOL-Datei:
260415-63-2.mol

PD173955 Eigenschaften

Dichte
1.49
storage temp. 
Store at -20° C
Löslichkeit
≥22.15 mg/mL in DMSO with gentle warming
Aggregatzustand
White powder.

Sicherheit

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 Händler.

Global( 94)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
Capot Chemical Co.,Ltd.
571-85586718 +8613336195806
sales@capotchem.com China 29797 60
ATK CHEMICAL COMPANY LIMITED
+undefined-21-51877795
ivan@atkchemical.com China 32480 60
Hubei Jusheng Technology Co.,Ltd.
18871490254
linda@hubeijusheng.com CHINA 28180 58
BOC Sciences
+1-631-485-4226
inquiry@bocsci.com United States 19553 58
CONIER CHEM AND PHARMA LIMITED
+8618523575427
sales@conier.com China 49390 58
Dideu Industries Group Limited
+86-29-89586680 +86-15129568250
1026@dideu.com China 29067 58
Hefei Hirisun Pharmatech Co., Ltd
+8615056975894
shawn@hirisunpharm.com CHINA 9923 58
InvivoChem
+1-708-310-1919 +1-13798911105
sales@invivochem.cn United States 6393 58
LEAP CHEM CO., LTD.
+86-852-30606658
market18@leapchem.com China 24738 58
TargetMol Chemicals Inc.
+1-781-999-5354
support@targetmol.com United States 19973 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
  • 260415-63-2
  • Inhibitors
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