Ki8751

Cat. No.: HY-12038 Purity: 99.17%: FAQs
Data Sheet SDS COA Handling Instructions

Ki8751 is a potent VEGFR2 inhibitor with an IC₅₀ of 0.9 nM.

For research use only. We do not sell to patients.

Ki8751 Chemical Structure

CAS No. : 228559-41-9

Size	Price	Stock	Quantity
Solution
10 mM * 1 mL in DMSO	USD 111	In-stock	Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL ready for reconstitution	USD 111	In-stock	Estimated Time of Arrival: December 31
Solid
10 mg	USD 101	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 416	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 733	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 3 publication(s) in Google Scholar

2 Publications Citing Use of MCE Ki8751

: Ki8751 purchased from MCE. Usage Cited in: Cell Death Dis. 2018 Sep 24;9(10):982. [Abstract]; Western blot is performed to detect the expression of VEGFR2, p-VEGFR2, Akt, p-Akt, mTOR, p-mTOR, E-cadherin, Vimentin, and N-cadherin after adding Ki8751 to HCT116, and HCT8 cells.

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

Ki8751 is a potent VEGFR2 inhibitor with an IC₅₀ of 0.9 nM.

IC₅₀ & Target^[1]

VEGFR2

0.9 nM (IC₅₀)

In Vitro

Ki8751 inhibits VEGFR-2 phosphorylation at an IC₅₀ value of 0.90 nM, and also inhibits the PDGFR family members such as PDGFRR and c-Kit at 67 nM and 40 nM, respectively. However, Ki8751 does not have any inhibitory activity against other kinases such as EGFR, HGFR, InsulinR and others even at 10000 nM. Ki8751 suppresses the growth of the VEGF-stimulated human umbilical vein endothelial cell (HUVEC) on a nanomolar level^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Ki8751 shows 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 and also shows 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^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

469.41

Appearance

Solid

Formula

C₂₄H₁₈F₃N₃O₄

CAS No.

228559-41-9

SMILES

COC1=CC2=C(C=CN=C2C=C1OC)OC3=CC=C(C(F)=C3)NC(NC4=CC=C(C=C4F)F)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : ≥ 92 mg/mL (195.99 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1303 mL	10.6517 mL	21.3033 mL
5 mM	0.4261 mL	2.1303 mL	4.2607 mL
10 mM	0.2130 mL	1.0652 mL	2.1303 mL

*Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: 2.5 mg/mL (5.33 mM); Suspended solution; Need ultrasonic
2.

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (5.33 mM); Suspended solution; Need ultrasonic
3.

Add each solvent one by one: 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.33 mM); Clear solution

*All of the co-solvents are available by MCE.

Purity & Documentation

Purity: 99.17%

Select Batch:

Data Sheet (281 KB) SDS (251 KB)

COA (253 KB) LCMS (91 KB)

Handling Instructions (2659 KB)

References

[1]. Kubo K, et al. 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. J Med Chem, 2005, 48(5), 1359-1366. [Content Brief]

Kinase Assay ^[1]	VEGFR-2 kinase assay is described below; GST-fusion proteins of KDR (Flk-1: cytoplasmic domain) are produced in the baculo-virus expression system. GST-KDR is premixed with a serial dilution of Ki8751 in the kinase buffer. The kinase reaction is initiated by the addition of 2 µM ATP in a solution of MnCl₂. After 20 min incubation at room temperature, the reaction is stopped with an addition of EDTA. Phosphorylation levels of GST-KDR are detected by immunoblotting with anti-phosphotyrosine monoclonal antibodies (PY20) and detected by ECL fluorography^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	HUVECs are placed at a density of 4000 cells/200 µL/well on collagene type I precoated 96-well plates in M199 medium with 5% fetal bovine serum (FBS). After 24 h, the cells are incubated for 1 h in the presence or absence of Ki8751; then the cells are stimulated by rhVEGF (20 ng/mL). The cultures are incubated at 37 °C for 72 h, then pulsed with 1 µCi/well [³H]thymidine and reincubated for 14 h. Cells are assayed for the incorporation of tritium using a beta counter^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice: The effects of Ki8751 on tumor growth is tested against various tumors, human stomach carcinoma (St-4), human lung carcinoma (LC-6), human colon carcinoma (DLD-1) and human melanoma (A375), using human tumor xenografts in nude mice. Ki8751 is administered orally to mice in the experimental groups once a day for 9 consecutive days at 5 mg/kg, and the vehicle is administered to control animals. Tumor volumes are monitored twice weekly^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Kubo K, et al. 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. J Med Chem, 2005, 48(5), 1359-1366. [Content Brief]

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Keywords:

Ki8751228559-41-9Ki 8751Ki-8751VEGFRVascular endothelial growth factor receptorInhibitorinhibitorinhibit

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Ki8751

Customer Review

2 Publications Citing Use of MCE Ki8751

Featured Recommendations

•Related Screening Libraries:

View All VEGFR Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

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The molarity calculator equation

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