GNE-9815 |
| Catalog No.GC65949 |
GNE-9815(화합물 7)는 경구 생체이용률이 우수한 매우 선택적인 범RAF 억제제입니다. 821d96072c2d58d8970e76f526b0f6b8GNE-9815는 CRAF 및 BRAF에 대해 각각 0.062 및 0.19nM의 Ki 값을 나타냅니다. 821d96072c2d58d8970e76f526b0f6b8GNE-9815는 MEK 억제제 Cobimetinib(HY-13064)와 결합하여 MAPK 경로의 상승적 조절을 보여줍니다. 821d96072c2d58d8970e76f526b0f6b8GNE-9815는 KRAS 돌연변이 암 연구에 사용할 수 있습니다.821d96072c2d58d8970e76f526b0f6b8
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2729996-45-4
Sample solution is provided at 25 µL, 10mM.
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GNE-9815 (compound 7) is a highly selective, pan-RAF inhibitor with good oral bioavailability. GNE-9815 exhibits Ki values of 0.062 and 0.19 nM for CRAF and BRAF, respectively. GNE-9815 combines with MEK inhibitor Cobimetinib (HY-13064) shows synergistic modulation of MAPK pathway. GNE-9815 can be used in studies of KRAS mutant cancers[1].
GNE-9815 shows synergistic activity in KRAS mutant A549 and HCT116 cancer cells in combination with the MEK inhibitor Cobimetinib[1].
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[1].
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[1].
| Animal Model: | Female NCR nude mice (6 to 8-week-old; 24-26 g; HCT116 xenograft mice model)[1]. |
| 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)[1]. |
| Dosage: | 1 mg/kg (for i.v.); 5 mg/kg (for p.o.). |
| Administration: | Intravenous injection or oral administration; single. |
| Result: | Exhibited CLb, Vdss and t1/2 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). |
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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