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(Z)-Orantinib

Name: (Z)-Orantinib
Brand: TargetMol
SKU: T9684
Price: 52 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T9684Cas No. 210644-62-5

Alias (Z)-TSU-68, (Z)-TSU68, (Z)-SU-6668, (Z)-SU6668

(Z)-Orantinib ((Z)-SU6668) is an effective, selective, orally active, ATP-competitive inhibitor of Flk-1/KDR, PDGFRβ, and FGFR1 with IC₅₀ values of 2.1, 0.008, and 1.2 μM, respectively. As a potent anti-angiogenic and anti-tumor compound, (Z)-Orantinib ((Z)-SU6668) induces significant regression in established tumors. (Z)-Orantinib serves as a valuable tool for investigating tumor angiogenesis inhibition mechanisms, tumor microenvironment regulation, and targeted anti-cancer strategy development, providing highly reliable experimental support for exploring solid tumor drug mechanisms and drug screening.

(Z)-Orantinib

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Purity: 98.05%

Catalog No. T9684Alias (Z)-TSU-68, (Z)-TSU68, (Z)-SU-6668, (Z)-SU6668Cas No. 210644-62-5

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$30	In Stock	In Stock
10 mg	$47	-	In Stock
25 mg	Preferential	-	In Stock
50 mg	Preferential	-	In Stock
1 mL x 10 mM (in DMSO)	$52	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:98.05%

Appearance:Solid

Color:Orange

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	(Z)-Orantinib ((Z)-SU6668) is an effective, selective, orally active, ATP-competitive inhibitor of Flk-1/KDR, PDGFRβ, and FGFR1 with IC₅₀ values of 2.1, 0.008, and 1.2 μM, respectively. As a potent anti-angiogenic and anti-tumor compound, (Z)-Orantinib ((Z)-SU6668) induces significant regression in established tumors. (Z)-Orantinib serves as a valuable tool for investigating tumor angiogenesis inhibition mechanisms, tumor microenvironment regulation, and targeted anti-cancer strategy development, providing highly reliable experimental support for exploring solid tumor drug mechanisms and drug screening.
Targets&IC50	FLK1/KDR:2.1 μM, FGFR1:1.2 μM, PDGFRβ:0.008 μM
In vitro	(Z)-Orantinib (5-15 minutes) inhibits Flk-1 transphosphorylation, FGFR1 transphosphorylation, and PDGFR autophosphorylation, with Ki values of 2.1 μM, 1.2 μM, and 0.008 μM, respectively [1]. (Z)-Orantinib (0.03-10 μM, 60 minutes) suppresses the increase in KDR tyrosine phosphorylation levels induced by VEGF in HUVECs [1]. (Z)-Orantinib shows dose-dependent inhibitory effects on the mitogenic activity of VEGF- and FGF-induced HUVECs, with IC50 values of 0.34 μM and 9.6 μM, respectively [1].
In vivo	(Z)-Orantinib (4-200 mg/kg, orally administered for 21 days) demonstrated dose-dependent inhibitory effects on the growth of A431 tumors in nude mice [1]. (Z)-Orantinib (75 mg/kg, administered intraperitoneally for 22 days) demonstrated significant inhibition of tumor angiogenesis and vascular formation in mice [1]. (Z)-Orantinib (200 mg/kg, orally administered for 11-27 days) significantly induced regression of established large A431 parazacco spilurus subsp. spilurus xenograft tumors in nude mice [1].
Synonyms	(Z)-TSU-68, (Z)-TSU68, (Z)-SU-6668, (Z)-SU6668

Chemical Properties

Molecular Weight	310.35
Formula	C₁₈H₁₈N₂O₃
Cas No.	210644-62-5
Smiles	C(=C\1/C=2C(NC1=O)=CC=CC2)\C3=C(C)C(CCC(O)=O)=C(C)N3

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 40 mg/mL (128.89 mM), Sonication is recommeded.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.2222 mL	16.1108 mL	32.2217 mL	161.1084 mL
5 mM	0.6444 mL	3.2222 mL	6.4443 mL	32.2217 mL
10 mM	0.3222 mL	1.6111 mL	3.2222 mL	16.1108 mL
20 mM	0.1611 mL	0.8055 mL	1.6111 mL	8.0554 mL
50 mM	0.0644 mL	0.3222 mL	0.6444 mL	3.2222 mL
100 mM	0.0322 mL	0.1611 mL	0.3222 mL	1.6111 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc