MGCD-265 analog

Name: MGCD-265 analog
Brand: MedChemExpress
SKU: HY-10991
Rating: 4.5 (1 reviews)

Cat. No.: HY-10991 Purity: 98.47%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

CAS No. : 875337-44-3

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 114	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 114	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 100	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 160	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 340	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 540	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

1 Publications Citing Use of MCE MGCD-265 analog

•Harvard Medical School LINCS LIBRARY

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View All Isoforms

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

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

VEGFR2

10 nM (IC₅₀)

c-Met

29 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
BTI-TN-5B1-4	IC₅₀	0.037 μM Compound: 5	Inhibition of GST-fused recombinant c-Met catalytic domain expressed in baculovirus-infected Trichoplusia ni Hi5 cells after 30 mins by DELFIA assay Inhibition of GST-fused recombinant c-Met catalytic domain expressed in baculovirus-infected Trichoplusia ni Hi5 cells after 30 mins by DELFIA assay	[PMID: 19211249]
HCC827	IC₅₀	0.08 μM Compound: 5	Antiproliferative activity against gefitinib resistant EGFR-mutated human HCC827 cells after 72 hrs by MTT assay Antiproliferative activity against gefitinib resistant EGFR-mutated human HCC827 cells after 72 hrs by MTT assay	[PMID: 28787156]
Sf9	IC₅₀	0.026 μM Compound: 5	Inhibition of GST-fused recombinant VGFR2 catalytic domain expressed in baculovirus-infected Sf9 cells after 10 mins by DELFIA assay Inhibition of GST-fused recombinant VGFR2 catalytic domain expressed in baculovirus-infected Sf9 cells after 10 mins by DELFIA assay	[PMID: 19211249]

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.

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 C_max (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%), C_max (0.14 μM/(mg/kg)), T_1/2 (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%), C_max (0.21 uM/(mg/kg)), T_1/2 (5.8 h).

Molecular Weight

517.60

Formula

C₂₆H₂₀FN₅O₂S₂

CAS No.

875337-44-3

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
10 mM	0.1932 mL	0.9660 mL	1.9320 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.75 mg/mL (5.31 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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

Purity: 98.47%

Select Batch:

Data Sheet (274 KB) SDS (252 KB)

COA (247 KB) LCMS (97 KB)

Handling Instructions (2659 KB)

References

[1]. Claridge S, et al. Discovery of a novel and potent series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases. Bioorg Med Chem Lett. 2008 May 1;18(9):2793-8. [Content Brief]

Complete Stock Solution Preparation Table

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

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.

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MGCD-265 analog

Customer Review

MGCD-265 analog Related Antibodies

1 Publications Citing Use of MCE MGCD-265 analog

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All VEGFR Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

MGCD-265 analog Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

MGCD-265 analog Related Classifications

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