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

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
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 180 In-stock
Solution
10 mM * 1 mL in DMSO USD 180 In-stock
Solid
2 mg USD 106 In-stock
5 mg USD 158 In-stock
10 mg USD 277 In-stock
50 mg USD 858 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

MGCD-265 analog Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE MGCD-265 analog

View All VEGFR Isoform Specific Products:

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

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

MGCD-265 analog Related Antibodies
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].

MedChemExpress (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.
Appearance

Solid

Color

White to off-white

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (193.20 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9320 mL 9.6600 mL 19.3199 mL 48.2998 mL
5 mM 0.3864 mL 1.9320 mL 3.8640 mL 9.6600 mL
10 mM 0.1932 mL 0.9660 mL 1.9320 mL 4.8300 mL
15 mM 0.1288 mL 0.6440 mL 1.2880 mL 3.2200 mL
20 mM 0.0966 mL 0.4830 mL 0.9660 mL 2.4150 mL
25 mM 0.0773 mL 0.3864 mL 0.7728 mL 1.9320 mL
30 mM 0.0644 mL 0.3220 mL 0.6440 mL 1.6100 mL
40 mM 0.0483 mL 0.2415 mL 0.4830 mL 1.2075 mL
50 mM 0.0386 mL 0.1932 mL 0.3864 mL 0.9660 mL
60 mM 0.0322 mL 0.1610 mL 0.3220 mL 0.8050 mL
80 mM 0.0241 mL 0.1207 mL 0.2415 mL 0.6037 mL
100 mM 0.0193 mL 0.0966 mL 0.1932 mL 0.4830 mL
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MGCD-265 analog Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MGCD-265875337-44-3MGCD265MGCD 265c-Met/HGFRVEGFRApoptosisVascular endothelial growth factor receptorGlesatinibreceptortyrosinekinasescellmigrationinvasionproliferationsurvivalmorphogenesisangiogenesisInhibitorinhibitorinhibit

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