1. Protein Tyrosine Kinase/RTK
    Apoptosis
  2. c-Met/HGFR
    VEGFR
    Apoptosis
  3. MGCD-265 analog

MGCD-265 analog 

Cat. No.: HY-10991 Purity: 98.57%
Handling Instructions

MGCD-265 analog is a potent and oral active inhibitor of c-Met and VEGFR2 tyrosine kinases, with IC50s of 29 nM and 10 nM, respectively. MGCD-265 analog has significant antitumor activity.

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

MGCD-265 analog Chemical Structure

MGCD-265 analog Chemical Structure

CAS No. : 875337-44-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 164 In-stock
Estimated Time of Arrival: December 31
2 mg USD 96 In-stock
Estimated Time of Arrival: December 31
5 mg USD 144 In-stock
Estimated Time of Arrival: December 31
10 mg USD 252 In-stock
Estimated Time of Arrival: December 31
50 mg USD 780 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Description

MGCD-265 analog is a potent and oral active inhibitor of c-Met and VEGFR2 tyrosine kinases, with IC50s of 29 nM and 10 nM, respectively. MGCD-265 analog has significant antitumor activity[1].

IC50 & Target[1]

VEGFR2

10 nM (IC50)

c-Met

29 nM (IC50)

In Vitro

MGCD-265 analog inhibits A549 cells migration and DU145 cells scattering, with IC50s of 0.4 μM and 0.08 μM, respectively, in HGF-driven cell migration and scattering assays[1].
MGCD-265 analog inhibits HUVEC ERK phosphorylation (IC50=0.03 μM) and HUVEC proliferation (IC50=0.006 μM) in VEGF-dependent cell-based assays[1].

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

In Vivo

MGCD-265 analog (20 mg/kg; p.o.) inhibits tumor growth inhibition on various human tumor models in mice[1].
MGCD-265 analog exhibits moderate oral bioavailability (rat 12%, dog 42%) and Cmax (rat 0.14, dog 0.21 uM/(mg/kg)) following oral administration (rat 5-25, dog 5 mg/kg)[1].
MGCD-265 analog exhibits reasonable terminal elimination half-lives (rat 1.2, dog 5.8 h) due to plasma clearance (rat 0.33, dog 1.1 L/(kg h)) following intravenous administration (rat 2.5, dog 0.8 mg/kg) [1].

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

Animal Model: Female Sprague-Dawley rats[1]
Dosage: 2.5 mg/kg for i.v.; 5-25 mg/kg for oral (Pharmacokinetic Analysis)
Administration: Intravenous injection and oral administration
Result: Oral bioavailability (12%), Cmax (0.14 μM/(mg/kg)), T1/2 (1.2 h),
Animal Model: Male beagle dogs
Dosage: 0.8 mg/kg for i.v.; 5 mg/kg for oral (Pharmacokinetic Analysis)
Administration: Intravenous administration and oral administration
Result: Oral bioavailability (42%), Cmax (0.21 uM/(mg/kg)), T1/2 (5.8 h).
Molecular Weight

517.60

Formula

C₂₆H₂₀FN₅O₂S₂

CAS No.

875337-44-3

SMILES

O=C(CC1=CC=CC=C1)NC(NC2=CC=C(C(F)=C2)OC3=C4C(C=C(S4)C5=CN(C=N5)C)=NC=C3)=S

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 : ≥ 100 mg/mL (193.20 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9320 mL 9.6600 mL 19.3199 mL
5 mM 0.3864 mL 1.9320 mL 3.8640 mL
10 mM 0.1932 mL 0.9660 mL 1.9320 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: ≥ 2.75 mg/mL (5.31 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.75 mg/mL (5.31 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.75 mg/mL (5.31 mM); Clear solution

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

MGCD-265 analogc-Met/HGFRVEGFRApoptosisVascular endothelial growth factor receptorMGCD-265GlesatinibreceptortyrosinekinasescellmigrationinvasionproliferationsurvivalmorphogenesisangiogenesisInhibitorinhibitorinhibit

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