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MGCD-265 analog

MGCD-265 analog

Item no.	S1361-5
Manufacturer	Selleckchem
CASRN	875337-44-3
Amount	5 mg
Quantity options	10 mg 1 g 10 g 10 mM/1 mL 200 mg 5 mg 50 mg 5 g
Category	Oncology Neuroscience Neural Lineage Markers Neuroinflammation Metabolism Diabetes Neural Transcription Factors Neural Signaling Inhibitors & Compound Libraries Small Molecules By Organ Lung Cancer Bladder Cancer
Type	Inhibitors
Specific against	other
Smiles	CN1C=C(N=C1)C2=CC3=NC=CC(=C3S2)OC4=C(C=C(C=C4)NC(=S)NC(=O)CC5=CC=CC=C5)F
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	875337-44-3'
Similar products	MGCD-265
Available
Manufacturer - Targets	MET
Storage Conditions	2 years -80 in solvent
Molecular Weight	517, 6
Administration	Orally
Animal Models	Mice (CD-1 nude) xenograft models of MKN45, U87MG, MDA-MB-231, COLO205, and A549 cells
Cell lines	HCT116, MDA-MB-231, SNU-5, and MKN45 cells
Clinical Trials	A Phase I clinical trial of MGCD-265 in advanced malignancies has been completed. Currently, MGCD-265, in combination of erlotinib or docetaxel, is under investigation in a Phase I/II clinical trial for advanced malignancies or non-small cell lung cancer.
Concentrations	0â€“5 uM
Dosages	20 mg/kgâ€“60 mg/kg
IC50	1 nM, 1 nM, 1 nM, 1 nM, 1 nM, 1 nM
In vitro	MGCD-265 is a multi-target inhibitor of receptor tyrosine kinases. MGCD-265 potently inhibits Met, MetY1235D, MetM1250T, VEGFR1, VEGF2, VEGF3, Ron, and Tie2, with IC50 values ranging from 1 nM to 7 nM. [1] MGCD-265 inhibits cell proliferation both in c-Met-driven tumor cells (MKN45, MNNG-HOS, and SNU-5) and in non-c-Met-driven tumor cells (HCT116 and MDA-MB-231), with IC50 values of 6 nMâ€“30 nM and 1 uMâ€“3 uM, respectively. In serum starved MKN45 cells, MGCD-265 (40 nMâ€“5 uM) effectively inhibits c-Met phosphorylation and its downstream signaling pathways, including Erk, Akt, Stat3, and Fak. MGCD-265 (6 nMâ€“1 uM) also induces apoptosis in MKN45 cells. [2]
In vivo	In c-Met-driven or non-c-Met-driven mice xenograft models of MKN45, U87MG, MDA-MB-231, COLO205, and A549 tumor cells, MGCD-265 (20 mg/kgâ€“60 mg/kg) inhibits tumor growth and c-Met signaling. MGCD-265 (40 mg/kg) also downregulates genes involved in angiogenesis, including VEGF and IL-8, both in tumor and plasma of mice with U87MG xenograft. MGCD-265 also inhibits the plasma level of shed-Met. [2]
Incubation Time	72 hours
Method	Cells are treated with MGCD-265 for 72 hours and cell number is determined as a function of mitochondrial activity, following incubation with MTT for 4 hours.
Solubility (25C)	DMSO 104 mg/mL, Water <1 mg/mL, Ethanol <1 mg/mL
Information	MGCD-265 is a potent, multi-target and ATP-competitive inhibitor of c-Met and VEGFR1/2/3 with IC50 of 1 nM, 3 nM/3 nM/4 nM, respectively; also inhibits Ron and Tie2. Phase 1/2.

Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.

All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.

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S1361-5-datasheet.pdf

S1361-5-safety-datasheet.pdf