PD173955

ChemicalBook > CAS DataBase List > PD173955

Product Name: PD173955
CAS No.: 260415-63-2
Chemical Name: PD173955
Synonyms: 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
Molecular Formula: C21H16Cl2N4OS
Formula Weight: 443.35
MOL File: 260415-63-2.mol

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PD173955 Property

Density: 1.49
storage temp.: Store at -20° C
solubility: ≥22.15 mg/mL in DMSO with gentle warming
form: White powder.

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ApexBio Technology

Product number: A8812
Product name: PD173955
Packaging: 1unit
Price: $28
Updated: 2021/12/16

ApexBio Technology

Product number: A8812
Product name: PD173955
Packaging: 5mg
Price: $138
Updated: 2021/12/16

Adipogen Life Sciences

Product number: SYN-1061-M005
Product name: PD-173955
Purity: ≥95%
Packaging: 5mg
Price: $297
Updated: 2021/12/16

American Custom Chemicals Corporation

Product number: BRS0000356
Product name: PD-173955
Purity: 95.00%
Packaging: 1MG
Price: $308.7
Updated: 2021/12/16

ChemScene

Product number: CS-3550
Product name: PD173955
Purity: 98.88%
Packaging: 10mg
Price: $336
Updated: 2021/12/16

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PD173955 Chemical Properties,Usage,Production

Definition

ChEBI: PD173955 is a dichlorobenzene, a methyl sulfide, a pyridopyrimidine and an aryl sulfide. It has a role as a tyrosine kinase inhibitor.

Biological Activity

pd173955 is a potent inhibitor of bcr-abl, src and yes with ic50 value of 1-2 nm, 300 nm and 175 nm, respectively [1-3].bcr-abl is a protein tyrosine kinase which has oncogenic potential. src is an enzyme and plays an important role in a variety of cancer cells survival, angiogenesis, proliferation and invasion pathways. yes is a proto-oncogene tyrosine-protein kinase smf belongs to the src kinase family [1-3].pd173955 is a potent bcr-abl, src and yes inhibitor. when tested with cml cd34+ gm progenitors, pd173955 inhibited kl-dependent proliferation at an ic50 value of 50 nm and gm-csf-dependent cell growth at an ic50 value of 1μm and the maximum inhibition was achieved at the dose of 25 nm. it was shown that pd173955 reduced the fractions of cells in g2-m phase and increased the cells in g1 phase with significant difference [2]. in ht29 cells, pd173955 treatment inhibited src auot-phosphorylation in a dose dependent manner. further, pd173955 showed inhibition on cell growth with ic50 value of 800 nm without morphologic changes and high concentrations arrested cell cycle at the m phase [1]. when tested with bcr-abl-depedent cell lines k562 and rwleu4, pd173955 showed inhibition on cell proliferation with the ic50 value of 35 and 10 nm, respectively and arrested cell cycle in g1 phase at the low nanomolar [3].

Enzyme inhibitor

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

References

[1]. windham, t.c., et al., src activation regulates anoikis in human colon tumor cell lines. oncogene, 2002. 21(51): p. 7797-807.
[2]. strife, a., et al., 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. 1(3): p. 176-85.
[3]. wisniewski, d., et al., characterization of potent inhibitors of the bcr-abl and the c-kit receptor tyrosine kinases. cancer res, 2002. 62(15): p. 4244-55.

PD173955 Preparation Products And Raw materials

Raw materials

Preparation Products

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260415-63-2, PD173955Related Search:

PD 166285 PD 0325901 PD 166793 PD 98059 PD184352 PD318088 Phenylsilane Benzeneruthenium(II) chloride dimer Phenyltrichlorosilane Bindarit PLX-4720 Fostamatinib Dasatinib SB 203580 Foretinib (GSK1363089)

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