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2018年5月6日星期日

Original: LY3009120 1454682-72-4, stock more than 100g

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Description: LY3009120, also known as DP-4978, is potent and selective pan-RAF inhibitor with potential anticancer activity. LY3009120 showed activities against BRaf or Ras mutant tumor cells . LY3009120 binds to ARaf, BRaf and CRaf isoforms with similar affinity in cells with activating mutations of BRaf or KRas. LY3009120 induces minimal paradoxical pathway activation in NRas or KRas mutant cells. LY3009120 inhibits MEK phosphorylation and cell proliferation in vitro, and exhibits anti-tumor activity in multiple xenograft models carrying mutations in BRaf, NRas or KRas.

Name: LY3009120 
CAS#: 1454682-72-4 
Chemical Formula: C23H29FN6O 
Exact Mass: 424.23869 
Molecular Weight: 424.52 
Elemental Analysis: C, 65.07; H, 6.89; F, 4.48; N, 19.80; O, 3.77

Synonym: LY3009120; LY-3009120; LY 3009120; DP4978; DP 4978; DP-4978.
IUPAC/Chemical Name: 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea
InChi Key: HHCBMISMPSAZBF-UHFFFAOYSA-N
InChi Code: InChI=1S/C23H29FN6O/c1-13-9-18(24)19(29-22(31)26-8-7-23(3,4)5)11-16(13)17-10-15-12-27-21(25-6)30-20(15)28-14(17)2/h9-12H,7-8H2,1-6H3,(H2,26,29,31)(H,25,27,28,30)
SMILES Code: O=C(NC1=CC(C2=CC3=CN=C(NC)N=C3N=C2C)=C(C)C=C1F)NCCC(C)(C)C
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.
Storage Condition: 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, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
Harmonized System Code: 293490

ADDITIONAL INFORMATION
  LY3009120 is a potentially best-in-class inhibitor of three Raf isoforms and Raf dimer, with activity against tumor cells with BRaf, NRas or KRas mutations, as well as melanoma cells with acquired resistance to current BRaf therapies.