TIE-2/VEGFR-2 kinase-IN-2

Cat. No.: HY-12572 Purity: 99.79%: FAQs
Data Sheet SDS COA Handling Instructions

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TIE-2/VEGFR-2 kinase-IN-2 is a potent dual VEGFR2 and Tie-2 inhibitor with pIC₅₀ values of 8.61 and 8.56, respectively. TIE-2/VEGFR-2 kinase-IN-2 is an anti-angiogenic agent and can be used for cancer research.

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

TIE-2/VEGFR-2 kinase-IN-2 Chemical Structure

CAS No. : 501693-48-7

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 187	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 187	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 170	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 280	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 570	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 920	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1500	In-stock	Estimated Time of Arrival: December 31
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500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Tie2

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

Biological Activity
Purity & Documentation
References
Customer Review

Description

TIE-2/VEGFR-2 kinase-IN-2 is a potent dual VEGFR2 and Tie-2 inhibitor with pIC₅₀ values of 8.61 and 8.56, respectively^[1]. TIE-2/VEGFR-2 kinase-IN-2 is an anti-angiogenic agent and can be used for cancer research^[2].

IC₅₀ & Target^[1]

Tie2

8.56 nM (pIC₅₀)

VEGFR-2

Tie-2

Cellular Effect

Cell Line	Type	Value	Description	References
HFF	IC₅₀	2506 nM Compound: 8a	Cytotoxicity against human HFF cells after 3 days Cytotoxicity against human HFF cells after 3 days	[PMID: 17276055]
HT-29	IC₅₀	300 nM Compound: 3	Induction of necroptosis in human HT-29 cells assessed as increase in TNFalpha/AT-406/zVAD-FMK-induced LDH release preincubated with cells followed by TNFalpha/AT-406/zVAD-FMK addition measured after 16 to 20 hrs by CytoTox 96 nonradioactive cytotoxicity Induction of necroptosis in human HT-29 cells assessed as increase in TNFalpha/AT-406/zVAD-FMK-induced LDH release preincubated with cells followed by TNFalpha/AT-406/zVAD-FMK addition measured after 16 to 20 hrs by CytoTox 96 nonradioactive cytotoxicity	[PMID: 29485864]
HT-29	IC₅₀	5084 nM Compound: 8a	Cytotoxicity against human HT29 cells after 3 days Cytotoxicity against human HT29 cells after 3 days	[PMID: 17276055]
Sf9	IC₅₀	0.013 μM Compound: 27	Inhibition of human N-terminal His-GST-TEV-fused RIP1 kinase domain (1 to 375) autophosphorylation expressed in baculovirus infected insect Sf9 cells after 4 hrs by ADP-Glo luminescence assay Inhibition of human N-terminal His-GST-TEV-fused RIP1 kinase domain (1 to 375) autophosphorylation expressed in baculovirus infected insect Sf9 cells after 4 hrs by ADP-Glo luminescence assay	[PMID: 24900635]
Sf9	IC₅₀	0.063 μM Compound: 27	Displacement of (14-(2-{[3-({2-{[4-(cyanomethyl)phenyl]amino}-6-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-4-pyrimidinyl}amino)propyl]amino}-2-oxoethyl)-16,16,18,18-tetramethyl-6,7,7a,8a,9,10,16,18-octahydrobenzo[2'',3'']indolizino[8'',7'':5',6']pyrano[3',2': Displacement of (14-(2-{[3-({2-{[4-(cyanomethyl)phenyl]amino}-6-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-4-pyrimidinyl}amino)propyl]amino}-2-oxoethyl)-16,16,18,18-tetramethyl-6,7,7a,8a,9,10,16,18-octahydrobenzo[2'',3'']indolizino[8'',7'':5',6']pyrano[3',2':	[PMID: 24900635]
U-937	IC₅₀	0.25 μM Compound: 27	Inhibition of RIP1 in human U937 cells assessed as prevention of TNFalpha/zVAD.fmk-induced necrotic cell death preincubated for 30 to 60 mins followed by TNF-alpha induction measured after overnight incubation by Cell Titer-Glo luminescence assay Inhibition of RIP1 in human U937 cells assessed as prevention of TNFalpha/zVAD.fmk-induced necrotic cell death preincubated for 30 to 60 mins followed by TNF-alpha induction measured after overnight incubation by Cell Titer-Glo luminescence assay	[PMID: 24900635]

Molecular Weight

431.34

Formula

C₂₀H₁₃F₄N₅O₂

CAS No.

501693-48-7

Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CC(C(F)(F)F)=CC=C1F)NC(C=C2)=CC=C2C3=COC4=C3C(N)=NC=N4

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 : 50 mg/mL (115.92 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3184 mL	11.5918 mL	23.1836 mL
5 mM	0.4637 mL	2.3184 mL	4.6367 mL
10 mM	0.2318 mL	1.1592 mL	2.3184 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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Concentration _(final)

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In Vivo Dissolution Calculator

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Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.79%

Select Batch:

Data Sheet (276 KB) SDS (252 KB)

COA (255 KB) HNMR (144 KB) RP-HPLC (152 KB) LCMS (372 KB)

Handling Instructions (2659 KB)

References

[1]. Yasushi Miyazaki, et al. Orally active 4-amino-5-diarylurea-furo[2,3-d]pyrimidine derivatives as anti-angiogenic agent inhibiting VEGFR2 and Tie-2. Bioorg Med Chem Lett. 2007 Mar 15;17(6):1773-8. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.3184 mL	11.5918 mL	23.1836 mL	57.9589 mL
	5 mM	0.4637 mL	2.3184 mL	4.6367 mL	11.5918 mL
	10 mM	0.2318 mL	1.1592 mL	2.3184 mL	5.7959 mL
	15 mM	0.1546 mL	0.7728 mL	1.5456 mL	3.8639 mL
	20 mM	0.1159 mL	0.5796 mL	1.1592 mL	2.8979 mL
	25 mM	0.0927 mL	0.4637 mL	0.9273 mL	2.3184 mL
	30 mM	0.0773 mL	0.3864 mL	0.7728 mL	1.9320 mL
	40 mM	0.0580 mL	0.2898 mL	0.5796 mL	1.4490 mL
	50 mM	0.0464 mL	0.2318 mL	0.4637 mL	1.1592 mL
	60 mM	0.0386 mL	0.1932 mL	0.3864 mL	0.9660 mL
	80 mM	0.0290 mL	0.1449 mL	0.2898 mL	0.7245 mL
	100 mM	0.0232 mL	0.1159 mL	0.2318 mL	0.5796 mL