BenzaMide, 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, 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)- Basic information
- Product Name:
- BenzaMide, 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)-
- Synonyms:
-
- BenzaMide, N-[3-[1,4-dihy...
- GNF-7
- N-(4-Methyl-3-(1-methyl-7-((6-methylpyridin-3-yl)amino)-2-oxo-1,2-dihydropyrimido[4,5-d]pyrimidin-3(4H)-yl)phenyl)-3-(trifluoromethyl)benzamide
- 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
- BenzaMide, 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)-
- N-[4-methyl-3-[1-methyl-7-[(6-methylpyridin-3-yl)amino]-2-oxo-4H-pyrimido[4,5-d]pyrimidin-3-yl]phenyl]-3-(trifluoromethyl)benzamide
- GNF-7, >98%
- CS-1945
- CAS:
- 839706-07-9
- MF:
- C28H24F3N7O2
- MW:
- 547.53
- Mol File:
- 839706-07-9.mol
BenzaMide, 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)- Chemical Properties
- Density
- 1.404±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- insoluble in EtOH; insoluble in H2O; ≥5.48 mg/mL in DMSO
- form
- solid
- pka
- 12.82±0.70(Predicted)
- color
- White to off-white
BenzaMide, 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)- Usage And Synthesis
Uses
GNF 7 inhibits ras signaling, Ack1 and germinal center kinase (GCK). Also, it suppresses proliferation, and induces cell cycle arrest and apoptosis in leukemia cells harboring NRAS mutations. It is a COVID19-related research product.
Biological Activity
gnf-7 is the type-ii inhibitor of t315i-bcr-abl [1]. bcr-abl, constitutively activated tyrosine kinase, is an oncogene associated with chronic myelogenous leukemia (cml) and some cases ofacute lymphocytic leukemia in humans.
in vitro
gnf-7 showed excellent growth inhibitory activity against some human cancer cells. the ic50 of gnf-7is 0.005, 0.001, and 0.008 μm when tested in colo205, sw620, and trkc-ba/f3 cell line, respectively.gnf-7 showed little effect on hek293t cells, a normal cell line [1].after treated for 24h (7.5mg/kg qd or 15 mg/kg qd), gnf-7 significantly decreaseddisease burden in mice and prolonged overall survival compared to vehicle-controls [2].
in vivo
in acute myelogenous leukemia and lymphoblastic leukemia models, gnf-7 potently and selectively inhibited nras-dependent cells [2]. in thet315i-bcr-abl-ba/f3 cell line bioluminescent xenograft mouse model,oral administration of gnf-7 with 10or20mg/kgexhibited significant efficacy against t315i-bcr-abl without appreciable toxicity [1].
IC 50
the ic50 of gnf-7is 0.005, 0.001, and 0.008 μm in colo205, sw620, and trkc-ba/f3 cells, respectively.
storage
Store at -20°C
References
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]. journal of medicinal chemistry, 2010, 53(15): 5439-5448.nonami a, sattler m, weisberg e, et al. identification of novel therapeutic targets in acute leukemias with nras mutations using a pharmacologic approach[j]. blood, 2015, 125(20): 3133-3143.
BenzaMide, 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)-Supplier
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