Art. -Nr.: HY-10991

MGCD-265 analog

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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.

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Reinheit: 98.49%
CAS. Nr.: 875337-44-3
Formel: C₂₆H₂₀FN₅O₂S₂
Molecular Weight:517.60

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

MGCD-265 analog Chemical Structure

CAS. Nr.: 875337-44-3

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

VEGFR2

10 nM (IC₅₀)

c-Met

29 nM (IC₅₀)

Alle VEGFR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.4 μM Compound: 10a	Inhibition of c-Met dependent HGF-induced human A549 cell migration Inhibition of c-Met dependent HGF-induced human A549 cell migration	[PMID: 18434145]
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]
DU-145	IC₅₀	0.08 μM Compound: 10a	Inhibition of c-Met dependent HGF-induced human DU145 cell scattering Inhibition of c-Met dependent HGF-induced human DU145 cell scattering	[PMID: 18434145]
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]
HUVEC	IC₅₀	0.03 μM Compound: 10a	Inhibition of human VEGFR2-dependent ERK phosphorylation in HUVEC Inhibition of human VEGFR2-dependent ERK phosphorylation in HUVEC	[PMID: 18434145]
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]
Sf9	IC₅₀	10 nM Compound: 10a	Inhibition of GST tagged VEGFR2 expressed in Sf9 cells Inhibition of GST tagged VEGFR2 expressed in Sf9 cells	[PMID: 18434145]
Sf9	IC₅₀	26 nM Compound: 5	Inhibition of GST-tagged VEGFR expressed in Sf9 cells Inhibition of GST-tagged VEGFR expressed in Sf9 cells	[PMID: 19854051]
Sf9	IC₅₀	29 nM Compound: 10a	Inhibition of GST tagged c-Met expressed in Sf9 cells Inhibition of GST tagged c-Met expressed in Sf9 cells	[PMID: 18434145]
Sf9	IC₅₀	37 nM Compound: 5	Inhibition of GST-tagged c-Met expressed in Sf9 cells Inhibition of GST-tagged c-Met expressed in Sf9 cells	[PMID: 19854051]

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).

Chemical Information

CAS. Nr. 875337-44-3
Appearance Solid
Molecular Weight 517.60
Formel C₂₆H₂₀FN₅O₂S₂
Color Off-white to light yellow
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Lösungsmittel & Löslichkeit

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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Alle VEGFR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MGCD-265 analog Related Classifications

HY-10991 Related Classifications