1. Protein Tyrosine Kinase/RTK
  2. VEGFR

Ki8751 (Synonyms: Ki 8751; Ki-8751)

Cat. No.: HY-12038 Purity: 99.62%
Data Sheet SDS Handling Instructions

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.

For research use only. We do not sell to patients.
Ki8751 Chemical Structure

Ki8751 Chemical Structure

CAS No. : 228559-41-9

Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO $85 In-stock
10 mg $77 In-stock
50 mg $315 In-stock
100 mg $555 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Description

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. IC50 value: 0.9 nM [1] Target: VEGFR2 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 [1]. In human umbilical vein endothelial cells (HUVECs), Ki8751 (1 nM–100 nM) effectively decreases VEGF-stimulated cell proliferation and vasculature permeability [2]. In metastatic colorectal cancer (CRC) cells MIP, RKO, SW620, and SW480, but not in HCT116, Ki8751 (10 nM) increases cellular senescence [3]. 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 [1].

References
M.Wt

469.41

Formula

C₂₄H₁₈F₃N₃O₄

CAS No.

228559-41-9

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Ki8751
Cat. No.:
HY-12038
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