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Ki8751

Cat. No. M1995
Ki8751 Structure
Size Price Availability Quantity
10mg USD 90 In stock
50mg USD 300 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

Ki8751 is a potent, selective inhibitor of VEGFR-2 tyrosine kinase (IC50 = 0.9 nM). Ki8751 suppressed the growth of the VEGF-stimulated human umbilical vein endothelial cell (HUVEC) and inhibits tumor growth in vivo. Ki8751 also inhibited the PDGFR family members such as PDGFRalpha and c-Kit at 67 nM and 40 nM, respectively. Ki8751 (10 nM) increases cellular senescence in metastatic colorectal cancer (CRC) cells MIP, RKO, SW620 and SW480. Ki8751 showed significant antitumor activity against five human tumor xenografts such as GL07 (glioma), St-4 (stomach carcinoma), LC6 (lung carcinoma), DLD-1 (colon carcinoma) and A375 (melanoma) in nude mice. Ki8751 also showed complete tumor growth inhibition with the LC-6 xenograft in nude rats following oral administration once a day for 14 days at 5 mg/kg without any body weight loss.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 469.41
Formula C24H18F3N3O4
CAS Number 228559-41-9
Purity >98%
Solubility DMSO 40 mg/mL
Storage at -20°C
References

Inhibition of VEGF induces cellular senescence in colorectal cancer cells.
Hasan MR, et al. Int J Cancer. 2011 Nov 1;129(9):2115-23. PMID: 21618508.

Novel potent orally active selective VEGFR-2 tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of N-phenyl-N'-{4-(4-quinolyloxy)phenyl}ureas.
Kubo K, et al. J Med Chem. 2005 Mar 10;48(5):1359-66. PMID: 15743179.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Ki8751 supplier, VEGFR/PDGFR, inhibitors

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