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MGCD-265 analog - 10mM in DMSO, high purity , CAS No.875337-44-3(DMSO)

COA

Grade & Purity:

10mM in DMSO

Cas Number: 875337-44-3(DMSO)
Molecular Weight: 517.6

In stock

Item Number

M408439

Grouped product items
SKU	Size	Availability	Price	Qty
M408439-1ml	1ml	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$333.90

VEGFR3 Selective Inhibitors

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Compound libraries (12325)

Basic Description

Synonyms	N-[[[3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl]amino]thioxomethyl]-benzeneacetamide
Specifications & Purity	10mM in DMSO
Biochemical and Physiological Mechanisms	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.
Storage Temp	Store at -80°C
Shipped In	Ice chest + Ice pads This product requires cold chain shipping. Ground and other economy services are not available.
Product Description	Information MGCD-265 is a potent, multi-target and ATP-competitive inhibitor ofc-MetandVEGFR1/2/3withIC50of 1 nM, 3 nM/3 nM/4 nM, respectively; also inhibits Ron and Tie2. Phase 1/2. In vitro MGCD-265 is a multi-target inhibitor of receptor tyrosine kinases. MGCD-265 potently inhibits Met, Met^Y1235D, Met^M1250T, VEGFR1, VEGF2, VEGF3, Ron, and Tie2, with IC50 values ranging from 1 nM to 7 nM. 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 nM–30 nM and 1 μM–3 μM, respectively. In serum starved MKN45 cells, MGCD-265 (40 nM–5 μM) effectively inhibits c-Met phosphorylation and its downstream signaling pathways, including Erk, Akt, Stat3, and Fak. MGCD-265 (6 nM–1 μM) also induces apoptosis in MKN45 cells. 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/kg–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. Cell Data cell lines： Concentrations：0–5 μM Incubation Time：72 hours Powder Purity:≥99%

Product Properties

ALogP	6.037
hba_count	4
HBD Count	2
Rotatable Bond	8

Associated Targets(Human)

MET Tclin Hepatocyte growth factor receptor (4 Activities)

Discover Target: MET

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

SMO Tclin Smoothened homolog (2 Activities)

Discover Target: SMO

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

BCR Tclin Breakpoint cluster region protein (1 Activities)

Discover Target: BCR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KDR Tclin Vascular endothelial growth factor receptor 2 (4 Activities)

Discover Target: KDR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Names and Identifiers

Smiles	C[N]1C=NC(=C1)C2=CC3=NC=CC(=C3S2)OC4=CC=C(NC(=S)NC(=O)CC5=CC=CC=C5)C=C4F
Molecular Weight	517.6
Reaxy-Rn	11706462
Reaxys-RN_link_address	https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=11706462&ln=

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):

Analytical Chart:

Chemical and Physical Properties

Solubility	Solubility (25°C) In vitro DMSO: 54 mg/mL (199.79 mM);
DMSO(mg / mL) Max Solubility	104
DMSO(mM) Max Solubility	200.93
Water(mg / mL) Max Solubility	<1

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