| Identification | Back Directory | [Name]
GCN2iB | [CAS]
2183470-12-2 | [Synonyms]
GCN2iB
GCN2iB HCl salt
N-[3-[2-(2-Amino-5-pyrimidinyl)ethynyl]-2,4-difluorophenyl]-5-chloro-2-methoxy-3-pyridinesulfonamide
3-Pyridinesulfonamide, N-[3-[2-(2-amino-5-pyrimidinyl)ethynyl]-2,4-difluorophenyl]-5-chloro-2-methoxy- | [Molecular Formula]
C18H12ClF2N5O3S | [MDL Number]
MFCD32015941 | [MOL File]
2183470-12-2.mol | [Molecular Weight]
451.83 |
| Chemical Properties | Back Directory | [Boiling point ]
662.6±65.0 °C(Predicted) | [density ]
1.63±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 16.67 mg/mL (36.89 mM);Water : < 0.1 mg/mL (insoluble) | [form ]
Solid | [pka]
4.80±0.50(Predicted) | [color ]
Off-white to light yellow | [InChI]
InChI=1S/C18H12ClF2N5O3S/c1-29-17-15(6-11(19)9-23-17)30(27,28)26-14-5-4-13(20)12(16(14)21)3-2-10-7-24-18(22)25-8-10/h4-9,26H,1H3,(H2,22,24,25) | [InChIKey]
JGHVXJKGYJYWOP-UHFFFAOYSA-N | [SMILES]
C1(OC)=NC=C(Cl)C=C1S(NC1=CC=C(F)C(C#CC2=CN=C(N)N=C2)=C1F)(=O)=O |
| Hazard Information | Back Directory | [Uses]
N-[3-[2-(2-Amino-5-pyrimidinyl)ethynyl]-2,4-difluorophenyl]-5-chloro-2-methoxy-3-pyridinesulfonamide is an intermediate used in the preparation of heterocyclic compounds as GCN2 inhibitors. | [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 elicit potent antitumor activity (P=0.0002) with synergistic effects. In MV-4-11 and SU.86.86 xenografts, robust antitumor activity of the combination of GCN2iB and ASNase is observed with synergistic effect, respectively. ASNase/GCN2iB-treated tumors do not show significant growth even after drug cessation. The combination of ASNase and GCN2iB yield survival advantage compared with the vehicle treated control with synergistic effect[1]. | [IC 50]
eIF2 |
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