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HER2&FLT3

G-749 (1457983-28-6)

G-749 is a novel and potent FLT3 inhibitor with IC50 of 0.4 nM, 0.6 nM and 1 nM for FLT3 (WT), FLT3 (D835Y), and Mer, respectively, showing lower potency against other tyrosine kinases.

Not Intended for Therapeutic Use. For research use only.

CAS: 1457983-28-6 Category

G-749 (1457983-28-6) Description:

G-749 is a novel FLT3 inhibitor that showed potent and sustained inhibition of the FLT3 wild type and mutants including FLT3-ITD, FLT3-D835Y, FLT3-ITD/N676D, and FLT3-ITD/F691L in cellular assays. G-749 retained its inhibitory potency in various drug-resistance milieus such as patient plasma, FLT3 ligand surge, and stromal protection. Furthermore, it displayed potent antileukemic activity in bone marrow blasts from AML patients regardless of FLT3 mutation status, including those with little or only minor responses to AC220 or PKC412. Oral administration of G-749 yielded complete tumor regression and increased life span in animal models. Thus, G-749 appears to be a promising next-generation drug candidate for the treatment of relapsed and refractory AML patients with various FLT3-ITD/FLT3-TKD mutants and further shows the ability to overcome drug resistance (Blood. 2014 Apr 3;123(14):2209-19).

G-749 (1457983-28-6) Specifications:

Product Name G-749
Chemical Name G-749; 1457983-28-6; G749; UNII-B06W426B66; B06W426B66; 8-bromo-2-[(1-methylpiperidin-4-yl)amino]-4-(4-phenoxyanilino)-6H-pyrido[4,3-d]pyrimidin-5-one
Purity ≥98% (HPLC)
CAS Number 1457983-28-6
Molecular Formula C25H25BrN6O2
Molecular Weight 521.419 g/mol
Monoisotopic Mass 520.122 g/mol
InChIKey SXWMIXPJPNCXQQ-UHFFFAOYSA-N
InChi Code InChI=1S/C25H25BrN6O2/c1-32-13-11-17(12-14-32)29-25-30-22-20(26)15-27-24(33)21(22)23(31-25)28-16-7-9-19(10-8-16)34-18-5-3-2-4-6-18/h2-10,15,17H,11-14H2,1H3,(H,27,33)(H2,28,29,30,31)
SMILES O=C1NC=C(Br)C2=NC(NC3CCN(C)CC3)=NC(NC4=CC=C(OC5=CC=CC=C5)C=C4)=C21
Form Powder
Color N/A
Solubility  This drug may be formulated in DMSO
Storage Temp.  -20°C
Shelf life >2 years if stored properly
Handling Dry, dark
Application sustained inhibition of the FLT3

 


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RIDADR NONH for all modes of transport

References:

  • Lee HK, Kim HW, Lee IY, Lee J, Lee J, Jung DS, Lee SY, Park SH, Hwang H, Choi JS, Kim JH, Kim SW, Kim JK, Cools J, Koh JS, Song HJ. G-749, a novel FLT3 kinase inhibitor, can overcome drug resistance for the treatment of acute myeloid leukemia. Blood. 2014 Apr 3;123(14):2209-19. doi: 10.1182/blood-2013-04-493916. Epub 2014 Feb 14. PubMed PMID: 24532805; PubMed Central PMCID: PMC3975259.
  • Wu M, Li C, Zhu X.J Hematol Oncol. 2018 Dec 4;11(1):133. doi: 10.1186/s13045-018-0675-4. Review.PMID: 30514344 Free PMC Article
  • Lee HK, Kim HW, Lee IY, Lee J, Lee J, Jung DS, Lee SY, Park SH, Hwang H, Choi JS, Kim JH, Kim SW, Kim JK, Cools J, Koh JS, Song HJ.Blood. 2014 Apr 3;123(14):2209-19. doi: 10.1182/blood-2013-04-493916. Epub 2014 Feb 14.PMID: 24532805

1 review for G-749 (1457983-28-6)

  1. Cofttek

    Never had such good experience before,The G-749 (1457983-28-6) is high purity,also customer service is pretty nice !gotta try!!

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