Ki8751 - 10mM in DMSO , CAS No.228559-41-9

CAS: 228559-41-9 Cat. No.: K408947 Formula: C₂₄H₁₈F₃N₃O₄ Peso molecolare: 469.41

GRADE & PURITY 10mM in DMSO

Synonyms

N-​(2,​4-​difluorophenyl)​-​N'-​[4-​[(6,​7-​dimethoxy-​4-​quinolinyl)​oxy]​-​2-​fluorophenyl]​-urea

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Panoramica

Information

Ki8751 is a potent and selective inhibitor ofVEGFR2withIC50of 0.9 nM, >40-fold selective for VEGFR2 than c-Kit, PDGFRα and FGFR-2, little activity to EGFR, HGFR and InsR.
In vitro

Ki8751 potently and selectively inhibits VEGFR2 with IC50 of 0.9 nM. Ki8751 also inhibits PDGFRα, c-Kit, and FGFR-2, with much higher IC50 values (40 nM–170 nM). Except for these several kinases, Ki8751 doesn\'t disturb other kinases, including HGFR, EGFR, and InsulinR, even at 10 μM. In human umbilical vein endothelial cells (HUVECs), Ki8751 (1 nM–100 nM) effectively decreases VEGF-stimulated cell proliferation and vasculature permeability. In metastatic colorectal cancer (CRC) cells MIP, RKO, SW620, and SW480, but not in HCT116, Ki8751 (10 nM) increases cellular senescence.

In vivo

In nude mice bearing human tumor xenografts of GL07, St-4, LC6, DLD-1, and A375 cells, Ki8751 (20 mg/kg) inhibits tumor growth. In nude rat xenograft models of LC-6 cells, Ki8751 (5 mg/kg) completely inhibits tumor growth without affecting body weight.
Cell Data

cell lines：HCT116 cells

Concentrations：1 nM–100 nM

Incubation Time：1 hour

Powder Purity:≥98%

Specifications

Sinonimi

N-​(2,​4-​difluorophenyl)​-​N'-​[4-​[(6,​7-​dimethoxy-​4-​quinolinyl)​oxy]​-​2-​fluorophenyl]​-urea

Specifiche e purezza

10mM in DMSO

Meccanismi biochimici e fisiologici

Ki8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM, >40-fold selective for VEGFR2 than c-Kit, PDGFRα and FGFR-2, little activity to EGFR, HGFR and InsR.

Condizioni di conservazione di stoccaggio

Store at -80°C

Spedito in

Dry ice packs + Cold packs

Questo prodotto richiede spedizione a catena fredda. I servizi di terra e altri servizi economici non sono disponibili.

Tipo di azione

INHIBITOR

Nomi e identificatori

• Isomeri SMILES: COC1=CC2=C(C=CN=C2C=C1OC)OC3=CC(=C(C=C3)NC(=O)NC4=C(C=C(C=C4)F)F)F
• Peso molecolare: 469.41
• Reaxy-Rn: 9963965
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=9963965&ln=

Obiettivi associati (umani)

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

Discover Target: KDR

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

Proprietà chimiche e fisiche

• Solubilità: Solubility (25°C) In vitro DMSO: 50 mg/mL (197.84 mM)
• Indice di rifrazione: 1.66
• Punto di ebollizione (°C): 497.07° C at 760 mmHg
• Punto di fusione (°C): 235-238°C

Domande frequenti

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 228559-41-9, the molecular formula is C24H18F3N3O4, and the molecular weight is 469.41 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.