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

Glesatinib hydrochloride (Synonyms: MGCD265 hydrochloride)

Cat. No.: HY-19642A Purity: 98.25%
Handling Instructions

Glesatinib hydrochloride (MGCD265 hydrochloride) is an orally active, potent MET/SMO dual inhibitor. Glesatinib hydrochloride, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC).

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

Glesatinib hydrochloride Chemical Structure

Glesatinib hydrochloride Chemical Structure

CAS No. : 1123838-51-6

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10 mM * 1  mL in DMSO USD 462 In-stock
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1 mg USD 120 In-stock
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10 mg USD 450 In-stock
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25 mg USD 900 In-stock
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50 mg USD 1500 In-stock
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100 mg USD 2500 In-stock
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Description

Glesatinib hydrochloride (MGCD265 hydrochloride) is an orally active, potent MET/SMO dual inhibitor. Glesatinib hydrochloride, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC)[1][2].

IC50 & Target[1]

MET

 

In Vitro

Glesatinib hydrochloride (MGCD265 hydrochloride; 0.01-5 μM; for 72 hours) results in a dose-dependent inhibition of cancer cell growth and shows the low IC50 value of 0.08 μM on NSCLC H1299 cells[1].
Glesatinib hydrochloride (0.01, 0.1, 0.5, 1 μM) significantly increases by several-fold the percentage of apoptotic cells in NSCLC H1299 cells[1].
Glesatinib hydrochloride has the cytotoxicity to P-gp overexpressing cancer cells KB-C2, SW620/Ad300, HEK293/ABCB1, and their parent cells KB-3-1, SW620, HEK293 cells with the IC50s fell between 5 and 10 μM[1].
Glesatinib hydrochloride (1, 3 μM; 120 mins) increases the intracellular [3H]-Paclitaxel accumulation and inhibits [3H]-Paclitaxel efflux in cancer cell lines overexpressing P-gp[2].
Glesatinib hydrochloride (0-40 μM) stimulates the ATPase activity of P-gp transporters in a dose-dependent manner[2].

Cell Proliferation Assay[1]

Cell Line: NSCLC H1299 cells
Concentration: 0.01, 0.1, 1, 2, 5 μM
Incubation Time: For 72 hours
Result: Resulted in a dose-dependent inhibition of cancer cell growth and showed the lowest IC50 value of 0.08 μM.
In Vivo

Glesatinib hydrochloride (MGCD265 hydrochloride; 15 mg/kg/day; orally; 40 weeks) causes a significant decrease in tumor size[1].

Animal Model: 4−6-week old female balb/c athymic (nu/nu) mice with HCC827 NSCLC tumor xenografts[1]
Dosage: 15 mg/kg
Administration: Orally; daily; 40 weeks
Result: Caused a significant decrease in tumor size.
Clinical Trial
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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (76.20 mM; Need ultrasonic)

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.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (3.81 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (3.81 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (3.81 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 98.25%

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Keywords:

GlesatinibMGCD265MGCD 265MGCD-265TAM Receptorc-Met/HGFRTyro3AxlMerorallyMETSMOtyrosinekinaseP-glycoproteinP-gpmultidrugresistanceMDRnon-smallcelllungcancerNSCLCInhibitorinhibitorinhibit

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Glesatinib hydrochloride
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