An FLT3 kinase inhibitor
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G-749

Item No. 22139

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
8-bromo-2-[(1-methyl-4-piperidinyl)amino]-4-[(4-phenoxyphenyl)amino]-pyrido[4,3-d]pyrimidin-5(6H)-one
CAS Number
1457983-28-6
Molecular Formula
C25H25BrN6O2
Formula Weight
521.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 16 mg/mlDMF:PBS (pH 7.2)(1:3): 0.25 mg/mlDMSO: 3 mg/ml
λmax
261 nm
SMILES
BrC1=CNC(C2=C1N=C(NC3CCN(C)CC3)N=C2NC4=CC=C(OC5=CC=CC=C5)C=C4)=O
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)
InChi Key
SXWMIXPJPNCXQQ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $68

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    5 mg

    $228

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    10 mg

    $387

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    25 mg

    $722

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    Product Description

    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.1 It also inhibits growth of human leukemia cell lines that express FLT3-ITD mutant kinase (IC50s = 3.5 and 7.5 nM for MV4-11 and Molm-14 cells, respectively) but has no effect on cells that lack FLT3 expression or that express wild-type FLT3. G-749 reduces tumor growth and increases survival in a dose-dependent manner in MV4-11 and Molm-14 murine leukemia xenograft models. It reduces growth of bone marrow blasts derived from acute myeloid leukemia patients, showing more potent inhibition of blasts expressing the FLT3-ITD mutant receptor.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    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).