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Product introduction
GNE-9815 (compound 7) is a highly selective, pan- RAF inhibitor with good oral bioavailability. GNE-9815 exhibits K i values of 0.062 and 0.19 nM for CRAF and BRAF , respectively. GNE-9815 combines with MEK inhibitor Cobimetinib shows synergistic modulation of MAPK pathway. GNE-9815 can be used in studies of KRAS mutant cancers In Vitro GNE-9815 shows synergistic activity in KRAS mutant A549 and HCT116 cancer cells in combination with the MEK inhibitor Cobimetinib. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo GNE-9815 (15 mg/kg; p.o.; single) demonstrates synergistic MAPK pathway modulation when combines with the MEK inhibitor Cobimetinib in an HCT116 xenograft mouse model . GNE-9815 (5 mg/kg; p.o.; single) shows good oral bioavailability and (1 mg/kg; i.v.; single) exhibits low blood clearance, moderate volume of distribution, and short half-life . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female NCR nude mice (6 to 8-week-old; 24-26 g; HCT116 xenograft mice model) . Dosage: 15 mg/kg Administration: Intravenous injection or oral administration; single. Result: Resulted in pathway inhibition as demonstrated by partial inhibition of pRSK between 2 and 24 h, but more robust, albeit transient, inhibition of the downstream MAPK target genes, DUSP6 and SPRY4. Led to deeper inhibition of the downstream MAPK target genes DUSP6 and SPRY4, when combined with the MEK inhibitor Cobimetinib, with maximal inhibition at 8 h and with a more modest rebound in levels at 24 h, post final dose. Animal Model: Female NCR nude mice (6 to 8-week-old; 24-26 g) . Dosage: 1 mg/kg (for i.v.); 5 mg/kg (for p.o.). Administration: Intravenous injection or oral administration; single. Result: Exhibited CL b , V dss and t 1/2 values of 17 mL/min∙kg, 1.7 L/kg and 1.9 h, respectively. Showed good oral bioavailability with F% of 37%. (methylcellulose/Tween formulation). Form:Solid IC50& Target:CRAF 0.062 nM (Ki) Braf 0.19 nM (Ki)
Chinese name
GNE-9815
English name
GNE-9815
Chinese alias
-
English alias
-
CAS number
2729996-45-4
molecular formula
C26H22FN5O2
molecular weight
455.48 g/mol
Exact mass
≥98%
PSA
-
Logp
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Research chemical 98% 5mg

Research chemical 98% 5mg, complete specifications; suitable for production, research, laboratory testing and inspection; digital one-stop procurement platform for scientific materials.

item number:S59940-5mg
Product model:5mg
level: 98% 5mg
Lead Time:30days
sold 455 Items
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