G-749|CAS 1457983-28-6|DC Chemicals

Cas No.:	1457983-28-6
Chemical Name:	G-749, G749, G 749, CS-3343
Synonyms:	G-749, G749, G 749, CS-3343
SMILES:	CN1CCC(CC1)NC2=NC3=C(C(=O)NC=C3Br)C(=N2)NC4=CC=C(C=C4)OC5=CC=CC=C5
Formula:	C₂₅H₂₅BrN₆O₂
M.Wt:	521.409
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:	1. Lee, H.K., Kim, H.W., Lee, I.Y., et al. G-749, a novel FLT3 kinase inhibitor, can overcome drug resistance for the treatment of acute myeloid leukemia. Blood 123(14), 2209-2219 (2014).

Description:

G-749 is a novel FLT3 inhibitor that showed potent and sustained inhibition of the FLT3 wild type and mutants with IC50s of 0.4/0.6/3.5/7.5 nM for Wt Flt3/D835Y/MV4-11/Molm-14 respectively.G-749 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.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101
2018-0101
2018-0101

Cat. No.	Product name	Field of application
DC5197	Quizartinib (AC220)	Quizartinib (AC220) is a second-generation FLT3 inhibitor for Flt3(ITD/WT) with IC50 of 1.1 nM/4.2 nM, 10-fold more selective for Flt3 than KIT, PDGFRα, PDGFRβ, RET, and CSF-1R. Phase 1/2.
DC8522	KW-2449	KW 2449 is a multikinase inhibitor of FLT3, ABL, ABL-T315I, and Aurora kinase.
DC9286	K03861	K03861 is a type II CDK2 inhibitor with Kd of 50 nM, 18.6 nM, 15.4 nM, and 9.7 nM for CDK2(WT), CDK2(C118L), CDK2(A144C), and CDK2(C118L/A144C), respectlvely.
DC7792	G-749	G-749 is an inhibitor of Fms-like tyrosine receptor kinase 3 (FLT3) with IC50 values ranging from 2.1 to 38.1 nM for wild-type and mutant (constitutively active) FLT3s in Ba/F3 cells expressing recombinant receptors.
DC8164	Gilteritinib(ASP2215)	FLT3/AXL inhibitor
DC5159	CP-868596 (Crenolanib)	Crenolanib (CP-868596) is a potent and selective inhibitor of PDGFRα/β with Kd of 2.1 nM/3.2 nM, also potently inhibits FLT3, sensitive to D842V mutation not V561D mutation, >100-fold more selective for PDGFR than c-Kit, VEGFR-2, TIE-2, FGFR-2, EGFR, erbB