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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $77 | In Stock | |
5 mg | $178 | In Stock | |
10 mg | $288 | In Stock | |
25 mg | $576 | In Stock | |
50 mg | $825 | In Stock | |
100 mg | $1,130 | In Stock | |
1 mL x 10 mM (in DMSO) | $196 | In Stock |
Description | GCN2iB is an ATP-competitive inhibitor of a serine/threonine-protein kinase general control nonderepressible 2 (GCN2), with an IC50 of 2.4 nM. |
In vitro | GCN2iB shows an IC50 value of 2.4 nM for GCN2 and potent cellular activity. In a panel of 468 kinases, only GCN2 shows >99.5% inhibition, and three kinases (MAP2K5, STK10, and ZAK) show >95%inhibition at 1 μM GCN2iB, demonstrating high kinase selectivity. |
In vivo | In the antitumor activity study of the CCRF-CEM xenografts, ASNase or GCN2iB alone does not significantly affect tumor growth.Notably, a combination of ASNase and GCN2iB elicits potent antitumor activity (P=0.0002) with synergistic effects.In MV-4-11 and SU.86.86 xenografts, the robust antitumor activity of the combination of GCN2iB and ASNase is observed with a synergistic effect, respectively.ASNase/GCN2iB-treated tumors do not show significant growth even after drug cessation. |
Molecular Weight | 451.83 |
Formula | C18H12ClF2N5O3S |
Cas No. | 2183470-12-2 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 55 mg/mL (121.73 mM) H2O: < 0.1 mg/mL (insoluble) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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