1. Protein Tyrosine Kinase/RTK
  2. TAM Receptor
    c-Met/HGFR

Glesatinib hydrochloride (Synonyms: MGCD265 hydrochloride)

Cat. No.: HY-19642A Purity: >98.0%
Handling Instructions

Glesatinib hydrochloride is an inhibitor of the MET and Axl receptor tyrosine kinase pathways, which drive tumour growth when altered.

For research use only. We do not sell to patients.

Glesatinib hydrochloride Chemical Structure

Glesatinib hydrochloride Chemical Structure

CAS No. : 1123838-51-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 606 In-stock
Estimated Time of Arrival: December 31
1 mg USD 180 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

    Glesatinib hydrochloride purchased from MCE. Usage Cited in: Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093.

    Western blot analysis of selected MAPK and AKT/mTOR pathway components in Trametinib- and Temsirolimus-treated cells.

    Glesatinib hydrochloride purchased from MCE. Usage Cited in: Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093.

    Western blot analysis of selected MAPK and AKT/mTOR pathway components in Trametinib- and Temsirolimus-treated cells.
    • Biological Activity

    • Technical Information

    • Purity & Documentation

    Description

    Glesatinib hydrochloride is an inhibitor of the MET and Axl receptor tyrosine kinase pathways, which drive tumour growth when altered. Target: MET, Axl Glesatinib is an orally bioavailable, small-molecule, multitargeted tyrosine kinase inhibitor with potential antineoplastic activity. MGCD265 binds to and inhibits the phosphorylation of several receptor tyrosine kinases (RTKs), including the c-Met receptor (hepatocyte growth factor receptor); the Tek/Tie-2 receptor; vascular endothelial growth factor receptor (VEGFR) types 1, 2, and 3; and the macrophage-stimulating 1 receptor (MST1R or RON). Glesatinib is a tyrosine kinase inhibitor that is expected to potently and selectively target tumors in patients with driver alterations in MET (mutations and gene amplification) and Axl (rearrangements) that occur in approximately 8% of patients with non-small cell lung cancer (NSCLC). Glesatinib is being evaluated in a Phase 1b study in patients with solid tumors that have genetic alterations in MET or AXL genes. The Phase 2 trial in NSCLC patients with MET genetic alterations is underway to confirm and extend the data that supports the clinical benefit of Glesatinib in patients with driver mutations in MET. Genetic alterations in these targets have been implicated as drivers of tumor growth and disease progression in NSCLC, gastroesophageal cancer and other solid tumors. MET and Axl are also implicated as drivers of tumor progression in patients whose tumors have become resistant to EGFR inhibitors. Therefore, Mirati believes that the combination of Glesatinib with an EGFR inhibitor could potentially treat patients who have become resistant to agents targeting EGFR. Mirati retains worldwide rights to Glesatinib.

    Clinical Trial
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 28 mg/mL (42.67 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.5240 mL 7.6200 mL 15.2400 mL
    5 mM 0.3048 mL 1.5240 mL 3.0480 mL
    10 mM 0.1524 mL 0.7620 mL 1.5240 mL
    *Please refer to the solubility information to select the appropriate solvent.
    Molecular Weight

    656.17

    Formula

    C₃₁H₂₈ClF₂N₅O₃S₂

    CAS No.

    1123838-51-6

    SMILES

    O=C(NC(NC1=CC=C(OC2=C3C(C=C(C4=NC=C(CNCCOC)C=C4)S3)=NC=C2)C(F)=C1)=S)CC5=CC=C(F)C=C5.Cl

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    • 王娟入库 竞价 核磁确认为1个盐酸盐
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    Product Name:
    Glesatinib hydrochloride
    Cat. No.:
    HY-19642A
    Quantity:

    Glesatinib hydrochloride

    Cat. No.: HY-19642A