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JAK2 inhibitor G5-7
CAS No. 939681-36-4
JAK2 inhibitor G5-7( G5-7 )
Catalog No. M16724 CAS No. 939681-36-4
JAK2 inhibitor G5-7 is a small molecule, allosteric JAK2 inhibitor.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 1 mL x 10 mM in DMSO | 71 | In Stock |
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| 5MG | 65 | In Stock |
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| 10MG | 98 | In Stock |
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| 25MG | 181 | In Stock |
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| 50MG | 256 | In Stock |
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| 100MG | 359 | In Stock |
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| 200MG | 486 | In Stock |
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| 500MG | Get Quote | In Stock |
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| 1G | Get Quote | In Stock |
|
Biological Information
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Product NameJAK2 inhibitor G5-7
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NoteResearch use only, not for human use.
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Brief DescriptionJAK2 inhibitor G5-7 is a small molecule, allosteric JAK2 inhibitor.
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DescriptionJAK2 inhibitor G5-7 is a small molecule, allosteric JAK2 inhibitor that selectively inhibits JAK2-mediated phosphorylation and activation of EGFR and STAT3 by binding to JAK2; demonstrates inhibitor of U87MG/EGFR and U87MG/EGFRvIII with IC50 of 0.75 and 1.0 uM, arrests cell cycle at G2 phase in both U87MG/EGFRvIII and U87MG/EGFRvIII/PTEN cells; significantly inhibits EGFR Tyr1068 phosphorylation but has no effect on EGFR Tyr1045 phosphorylation; decreases GBM tumor volume and extends the life span of tumor-bearing nude mice after oral administration.
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In VitroG5-7 (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.Western Blot Analysis.Cell Line:U87MG/PTEN cells.Concentration:0-5 μM.Incubation Time:6 hours.Result:Blocked EGFR phosphorylation and cell cycle at G2 phase to inhibit cell proliferation.
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In VivoG5-7 (10 and 50 mg/kg, oral gavege) decreases VEGF secretion and exerts a potent antiangiogenic effect. Animal Model:Cells (4 × 106) in 100 μl of serum-free DMEM were inoculated subcutaneously into 5- to 6-week-old female nude mice.Dosage:10 and 50 mg/kg.Administration:Oral gavage.Result:Suppresses angiogenesis in tumors.
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SynonymsG5-7
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PathwayAngiogenesis
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TargetJAK
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RecptorJAK
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Research Area——
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Indication——
Chemical Information
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CAS Number939681-36-4
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Formula Weight383.395
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Molecular FormulaC22H19F2NO3
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 83.33 mg/mL (217.35 mM)
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SMILES——
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Chemical Nameethyl 3,5-bis((E)-2-fluorobenzylidene)-4-oxopiperidine-1-carboxylate
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
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PF-06651600
PF-06651600 is a novel potent, selective JAK3 inhibitor with IC50 of 0.346 nM, displays >1,000-fold selectivity over JAK1 and JAK2; inhibits Th1 and Th17 cell differentiation and function, reduces disease pathology in rat adjuvant-induced arthritis as well as in mouse experimental autoimmune encephalomyelitis models; selectively targets γc cytokine pathways while preserving JAK1-dependent anti-inflammatory signaling such as the IL-10 suppressive functions following LPS treatment in macrophages and the suppression of TNFα and IL-1β production in IL-27-primed macrophages.Rheumatoid ArthritisPhase 2 Clinical
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AS 2553627
AS 2553627 (AS2553627)?is a novel potent, selective pan-JAK inhibitor.
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S-Ruxolitinib
Ruxolitinib (INCB018424) is the first potent selective JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM in cell-free assays.
