MGCD-265 analog

ArtNr	S1361-10
Hersteller	Selleckchem
CAS-Nr.	875337-44-3
Menge	10 mg
Quantity options	10 mg 1 g 10 g 10 mM/1 mL 200 mg 5 mg 50 mg 5 g
Kategorie	Oncology Neuroscience Neural Lineage Markers Neuroinflammation Metabolism Diabetes Neural Transcription Factors Neural Signaling Inhibitors & Compound Libraries Small Molecules By Organ Lung Cancer Bladder Cancer
Typ	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
Lieferbar
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.

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