G5-7 - ≥99% , CAS No.939681-36-4

CAS: 939681-36-4 Cat. No.: G646574 分子式: C₂₄H₂₃F₂NO₃ 分子量: 411.4 PubChem CID: 73553353

グレード＆純度 ≥99%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

概要

G5-7, an orally active and allosteric JAK2 inhibitor, selectively inhibits JAK2 mediated phosphorylation and activation of EGFR (Tyr 1068 ) 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

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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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.

In Vivo

G5-7 (10 and 50 mg/kg, oral gavege) decreases VEGF secretion and exerts a potent antiangiogenic effect . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Cells (4 × 10 6 ) 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.

Form:Solid

IC50& Target:JAK2

仕様

仕様と純度

≥99%

生化学的・生理学的メカニズム

G5-7, an orally active and allosteric JAK2 inhibitor, selectively inhibits JAK2 mediated phosphorylation and activation of EGFR (Tyr 1068 ) and STAT3 by binding to JAK2 . G5-7 induces cell cycle arrest, apoptosis and possesses antiangiogenic effect. G5-7

保管条件

Store at -20°C

入荷

Ice chest + Ice pads

この製品は冷冷この冷このこの製品の運送が必要です。地上およびその他の経済サービスは利用できません。

アクションタイプ

INHIBITOR

純度

≥99%

名前と識別子

カノニカル・スマイル

CC(C)(C)OC(=O)N1CC(=CC2=CC=CC=C2F)C(=O)C(=CC3=CC=CC=C3F)C1

IUPAC Name

tert-butyl (3Z,5Z)-3,5-bis[(2-fluorophenyl)methylidene]-4-oxopiperidine-1-carboxylate

InChIKey

MCSPIRBNMDODQP-BKHHGCLFSA-N

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-

異性体SMILES

CC(OC(=O)N1C/C(=C/C2=CC=CC=C2F)/C(=O)/C(=C\C3=CC=CC=C3F)/C1)(C)C

PubChem CID

73553353

分子量

411.4

Taxonomic Classification

Taxonomy Tree

• Kingdom Organic compounds
  • Superclass Organoheterocyclic compounds
    • 分類 Piperidines
      • Subclass Piperidinecarboxylic acids and derivatives

• Kingdom: Organic compounds
• Superclass: Organoheterocyclic compounds
• 分類: Piperidines
• Subclass: Piperidinecarboxylic acids and derivatives
• Intermediate Tree Nodes: Not available
• Direct Parent: Piperidinecarboxylic acids
• Alternative Parents: Piperidinones Fluorobenzenes Aryl fluorides Carbamate esters Cyclic ketones Azacyclic compounds Organonitrogen compounds Organofluorides Organic oxides Hydrocarbon derivatives
• Molecular Framework: Aromatic heteromonocyclic compounds
• Substituents: Piperidinecarboxylic acid - Fluorobenzene - Halobenzene - Piperidinone - Aryl fluoride - Aryl halide - Monocyclic benzene moiety - Benzenoid - Carbamic acid ester - Ketone - Cyclic ketone - Azacycle - Hydrocarbon derivative - Organic oxide - Organooxygen compound - Organonitrogen compound - Organofluoride - Organohalogen compound - Organic oxygen compound - Organic nitrogen compound - Carbonyl group - Aromatic heteromonocyclic compound
• 説明: This compound belongs to the class of organic compounds known as piperidinecarboxylic acids. These are compounds containing a piperidine ring which bears a carboxylic acid group.
• External Descriptors: Not available

Data sources

1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.

DOI: 10.1186/s13321-016-0174-y

化学的性質と物理的性質

• 溶解度: DMSO : 83.33 mg/mL (217.35 mM; Need ultrasonic)

よくある質問

What is the purity of this product?

This product is supplied at ≥99% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.

How should this product be stored?

Store at ?20 °C. Freezer storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships in an insulated container with ice pads. Unpack on arrival and transfer it to the storage condition stated above.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 939681-36-4, the molecular formula is C24H23F2NO3, and the molecular weight is 411.4 g/mol. InChIKey MCSPIRBNMDODQP-BKHHGCLFSA-N.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.