Description
G5-7, an orally active and allosteric JAK2 inhibitor, selectively inhibits JAK2 mediated phosphorylation and activation of EGFR (Tyr1068) and STAT3 by binding to JAK2. G5-7 induces cell cycle arrest, apoptosis and possesses antiangiogenic effect. G5-7 has the potential for glioma study.
Product information
CAS Number: 939681-36-4
Molecular Weight: 411.44
Formula: C24H23F2NO3
Chemical Name: tert-butyl (3Z,5Z)-3,5-bis[(2-fluorophenyl)methylidene]-4-oxopiperidine-1-carboxylate
Smiles: CC(C)(C)OC(=O)N1C/C(=C/C2=CC=CC=C2F)/C(=O)/C(/C1)=C\C1=CC=CC=C1F
InChiKey: MCSPIRBNMDODQP-BKHHGCLFSA-N
InChi: InChI=1S/C24H23F2NO3/c1-24(2,3)30-23(29)27-14-18(12-16-8-4-6-10-20(16)25)22(28)19(15-27)13-17-9-5-7-11-21(17)26/h4-13H,14-15H2,1-3H3/b18-12-,19-13-
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 83.33 mg/mL (217.35 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
G5-7 (0-5 μM) inhibits EGFR tyrosine phosphorylation and downstream mTOR signaling and arrests the cell cycle at G2 phase. G5-7 does not directly inhibit EGFR activation. G5-7 (0-10 μM) comparably increases the abundance of markers (cleved-PARP and caspase 3) of apoptosis in parental LN229 cells and U87MG/EGFRvIII cells. G5-7 interacts with full-length JAK2. G5-7 significantly inhibits EGFR Tyr1068 phosphorylation but had no effect on EGFR Tyr1045 phosphorylation. G5-7 downregulates the downstream signaling of JAK by mTOR.
In Vivo:
G5-7 (10 and 50 mg/kg, oral gavege) decreases VEGF secretion and exerts a potent antiangiogenic effect.
Products are for research use only. Not for human use.
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