GCN2iB
GCN2iB Basic information
- Product Name:
- GCN2iB
- 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-
- inhibit,GCN-2iB,Inhibitor,GCN2iB,Eukaryotic Initiation Factor (eIF),Autophagy
- N-(3-((2-Aminopyrimidin-5-yl)ethynyl)-2,4-difluorophenyl)-5-chloro-2-methoxypyridine-3-sulfonamide
- N-(3-((2-Aminopyrimidin-5-yl)ethynyl)-2,4-difluorophenyl)-5-chloro-2-methoxypyridine-3-sulfonamide , GCN2iB
- GCN2iB, 10 mM in DMSO
- CAS:
- 2183470-12-2
- MF:
- C18H12ClF2N5O3S
- MW:
- 451.83
- Mol File:
- 2183470-12-2.mol
GCN2iB Chemical Properties
- 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)
- pka
- 4.80±0.50(Predicted)
- form
- Solid
- 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
GCN2iB Usage And Synthesis
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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