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)- Property

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

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Danger

Hazard statements

H301Toxic if swalloed

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P301+P310IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.

P321Specific treatment (see … on this label).

P330Rinse mouth.

P405Store locked up.

P501Dispose of contents/container to..…

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,Usage,Production

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.