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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 Safety Supplier Related

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
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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
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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

Shanghai Boyle Chemical Co., Ltd.
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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)-(839706-07-9)Related Product Information