A multi-kinase inhibitor
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GNF-7

Item No. 19918

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[3-[1,4-dihydro-1-methyl-7-[(6-methyl-3-pyridinyl)amino]-2-oxopyrimido[4,5-d]pyrimidin-3(2H)-yl]-4-methylphenyl]-3-(trifluoromethyl)-benzamide
CAS Number
839706-07-9
Molecular Formula
C28H24F3N7O2
Formula Weight
547.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMF:PBS(pH7.2) (1:2): 0.3 mg/mlDMSO: 2 mg/mlEthanol: 0.1 mg/ml
λmax
277 nm
SMILES
CC1=NC=C(NC2=NC=C(CN(C3=C(C)C=CC(NC(C4=CC(C(F)(F)F)=CC=C4)=O)=C3)C(N5C)=O)C5=N2)C=C1
InChi Code
InChI=1S/C28H24F3N7O2/c1-16-7-9-21(34-25(39)18-5-4-6-20(11-18)28(29,30)31)12-23(16)38-15-19-13-33-26(36-24(19)37(3)27(38)40)35-22-10-8-17(2)32-14-22/h4-14H,15H2,1-3H3,(H,34,39)(H,33,35,36)
InChi Key
SZNYUUZOQHNEKB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    GNF-7 is a multi-kinase inhibitor (IC50s = 25, 8, 61, 122, 136, and 133 nM for ACK1, GCK, Bcr-AblT315I, Bcr-AblE255V, Bcr-AblG250E, and c-Abl, respectively).1,2 It also inhibits several additional kinases in a panel by greater than 50% when used at a concentration of 10 μM.2 GNF-7 inhibits the growth of Ba/F3 cells transformed with wild-type Bcr-Abl, Bcr-AblT315I, Bcr-AblE255V, and Bcr-AblG250E (IC50s = <5 nM), as well as COLO 205 and SW625 cancer cells (IC50s = 1 and 5 nM, respectively) in vitro. In vivo, GNF-7 (10 and 20 mg/kg) reduces tumor growth in a Bcr-AblT315I Ba/F3 mouse xenograft model. It also reduces tumor volume in an OCI-AML3 mouse xenograft model when administered at a dose of 8 mg/kg.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Cho, H., Shin, I., Ju, E., et al. First SAR study for overriding NRAS mutant driven acute myeloid leukemia. J. Med. Chem. 61(18), 8353-8373 (2018).

    2. Choi, H.G., Ren, P., Adrian, F., et al. A type-II kinase inhibitor capable of inhibiting the T315I "gatekeeper" mutant of Bcr-Abl. J. Med. Chem. 53(15), 5439-5448 (2010).