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GSK1904529A

GSK1904529A structure

GSK1904529A 

structure
  • CAS No:

    1089283-49-7

  • Formula:

    C44H47F2N9O5S

  • Chemical Name:

    GSK1904529A

  • Synonyms:

    GSK1904529A;GSK1904529A : IGF-IR, IGF-IIR inhibitor;N-(2,6-Difluorophenyl)-5-[3-[2-[[5-ethyl-2-(methyloxy)-4-[4-[4-(methylsulfonyl)-1-piperazinyl]-1-piperidinyl]phenyl]amino]-4-pyrimidinyl]imidazo[1,2-a]pyridin-2-yl]-2-(methyloxy)benzamide;GSK 4529;N-(2,6-difluorophenyl)-5-(3-(2-(5-ethyl-2-methoxy-4-(4-(4-(methylsulfonyl)piperazin-1-yl)piperidin-1-yl)phenylamino)pyrimidin-4-yl)H-imidazo[1,2-a]pyridin-2-yl)-2-methoxybenzamide;N-(2,6-Difluorophenyl)-5-[3-[2-[[5-ethyl-2-(methyloxy)-4-[4-[4-(methylsulfonyl)-1-piperazinyl]-1-piperidinyl]phenyl]amino]-4-pyrimidinyl]imidazo[1,2-a]pyridin-2-yl]-2-(methyloxy)benzamide GSK 1904529A;GSK1904529A, >=98%;IGF-IR, IGF-IIR inhibitor

  • Categories:

    Pharmaceutical Intermediates  >  Heterocyclic Compound

Description

GSK1904529A is a selective inhibitor of IGF-1R and IR with IC50 of 27 nM and 25 nM, >100-fold more selective for IGF-1R/InsR than Akt1/2, Aurora A/B,B-Raf, CDK2, EGFR etc. IC50 value: 27/25 nM (IGF1R/IR) [1]Target: IGF1R/IRin vitro: GSK1904529A is a reversible, ATP-competitive inhibitor and has enzyme-inhibitor binding values against IGF-1R and IR with Ki of 1.6 nM and 1.3 nM, respectively. GSK1904529A potently inhibits the ligand-induced phosphorylation of IGF-1R and IR at concentration


N-(2,6-difluorophenyl)-5-[3-[2-[5-ethyl-2-methoxy-4-[4-(4-methylsulfonyl-1-piperazinyl)-1-piperidinyl]anilino]-4-pyrimidinyl]-2-imidazo[1,2-a]pyridinyl]-2-methoxybenzamide is a member of benzamides.

GSK1904529A Basic Attributes

851.98

851.338867

DTXSID70648776

Characteristics

155

6.8

1.39

1.672

Drug Information

GSK1904529A

GSK1904529A Use and Manufacturing

A selective inhibitor of IGF-1R and IR with IC50s of 27 nM and 25 nM, respectively.

Computed Properties

Molecular Weight:852.0
XLogP3:6.8
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:14
Rotatable Bond Count:12
Exact Mass:851.33889313
Monoisotopic Mass:851.33889313
Topological Polar Surface Area:155
Heavy Atom Count:61
Complexity:1530
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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