Cat. No.: HY-10517

Orantinib

(Synonyms: SU6668; TSU-68)

6 Cited Publications

Customer Review

Based on 6 publication(s) in Google Scholar

Orantinib (SU6668; TSU-68) is a multi-targeted receptor tyrosine kinase inhibitor with K_is of 2.1 μM, 8 nM and 1.2 μM for Flt-1, PDGFRβ and FGFR1, respectively.

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

Purity: 98.52%
CAS No.: 252916-29-3
Formula: C₁₈H₁₈N₂O₃
Molecular Weight:310.35

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Orantinib Chemical Structure

CAS No.: 252916-29-3

Size

Price

Stock

Quantity

Amount: USD 0.00

* Please select Quantity before adding items.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (6)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

Orantinib (SU6668; TSU-68) is a multi-targeted receptor tyrosine kinase inhibitor with K_is of 2.1 μM, 8 nM and 1.2 μM for Flt-1, PDGFRβ and FGFR1, respectively.

IC₅₀ & Target^[1]

PDGFRβ

8 nM (Ki)

FGFR1

1.2 μM (Ki)

Flt-1

2.1 μM (Ki)

All PDGFR Isoforms :

All VEGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
3T3	IC₅₀	1 μM Compound: 5b	Inhibition of Platelet-derived growth factor induced 3T3 cell proliferation Inhibition of Platelet-derived growth factor induced 3T3 cell proliferation	[PMID: 12646019]
HUVEC	IC₅₀	>50 μM Compound: SU-6668	Inhibition of rhFGF2-induced cellular proliferation of HUVEC Inhibition of rhFGF2-induced cellular proliferation of HUVEC	[PMID: 17618113]
HUVEC	IC₅₀	>50 μM Compound: SU-6668	Inhibition of rhFGF2-induced HUVEC proliferation Inhibition of rhFGF2-induced HUVEC proliferation	[PMID: 19110422]
HUVEC	IC₅₀	3.9 μM Compound: 51	Inhibition of VEGFR2 phosphorylation in HUVEC by chemiluminescence assay Inhibition of VEGFR2 phosphorylation in HUVEC by chemiluminescence assay	[PMID: 20403700]
MV4-11	IC₅₀	3.9 μM Compound: Orantinib	Antiproliferative activity against human MV4-11 cells after 72 hrs by Celltiter-Glo luminescent cell viability assay Antiproliferative activity against human MV4-11 cells after 72 hrs by Celltiter-Glo luminescent cell viability assay	[PMID: 29935772]
NIH3T3	IC₅₀	0.1 μM Compound: 51	Inhibition of PDGF-stimulated PDGFRbeta phosphorylation expressed in mouse NIH/3T3 cells by chemiluminescence assay Inhibition of PDGF-stimulated PDGFRbeta phosphorylation expressed in mouse NIH/3T3 cells by chemiluminescence assay	[PMID: 20403700]
NIH3T3	IC₅₀	0.3 μM Compound: 5b	Inhibition of PDGF-induced BrdU incorporation in 3T3 cells without bovine serum albumin Inhibition of PDGF-induced BrdU incorporation in 3T3 cells without bovine serum albumin	[PMID: 12646019]
NIH3T3	IC₅₀	16 μM Compound: 5b	Inhibition of PDGF-induced BrdU incorporation in 3T3 cells Inhibition of PDGF-induced BrdU incorporation in 3T3 cells	[PMID: 12646019]
NIH3T3	IC₅₀	16 μM Compound: 5b	Inhibition of PDGF-induced BrdU incorporation in 3T3 cells with 0.5% bovine serum albumin Inhibition of PDGF-induced BrdU incorporation in 3T3 cells with 0.5% bovine serum albumin	[PMID: 12646019]
NIH3T3	IC₅₀	2 μM Compound: 5b	Inhibition of Vascular endothelial growth factor receptor in 3T3 cells Inhibition of Vascular endothelial growth factor receptor in 3T3 cells	[PMID: 12646019]
NIH3T3	IC₅₀	36 μM Compound: 5b	Inhibition of PDGF-induced BrdU incorporation in 3T3 cells with 1% bovine serum albumin Inhibition of PDGF-induced BrdU incorporation in 3T3 cells with 1% bovine serum albumin	[PMID: 12646019]
NIH3T3	IC₅₀	49 μM Compound: 5b	Inhibition of PDGF-induced BrdU incorporation in 3T3 cells with 5% bovine serum albumin Inhibition of PDGF-induced BrdU incorporation in 3T3 cells with 5% bovine serum albumin	[PMID: 12646019]
NIH3T3	IC₅₀	9.5 μM Compound: 5b	Inhibition of PDGF-induced BrdU incorporation in 3T3 cells with 0.1% bovine serum albumin Inhibition of PDGF-induced BrdU incorporation in 3T3 cells with 0.1% bovine serum albumin	[PMID: 12646019]
Sf9	IC₅₀	28.4 μM Compound: R2C3, 30	Inhibition of human GST-fused ZAP-70 expressed in Sf9 cells Inhibition of human GST-fused ZAP-70 expressed in Sf9 cells	[PMID: 19674816]

In Vitro

Orantinib (SU6668; 0.03-10 μM) shows inhibitory activity against tyrosine phosphorylation of KDR in VEGF stimulated HUVECs, and also blocks PDGF-stimulated PDGFRβ tyrosine phosphorylation in NIH-3T3 cells overexpressing PDGFRβ. Orantinib (≥10 μM) inhibits acidic FGF-induced phosphorylation of the FGFR1 substrate 2. However, Orantinib (up to 100 μM) has no effect on EGF-stimulated EGFR tyrosine phosphorylation in NIH-3T3 cells overexpressing EGFR. Furthermore, Orantinib inhibits VEGF-driven and FGF-driven mitogenesis of HUVECs with mean IC₅₀ of 0.34 μM and 9.6 μM, respectively^[1]. In human myeloid leukemia MO7E cells, Orantinib (SU6668) inhibits the tyrosine autophosphorylation of stem cell factor (SCF) receptor, c-kit, with IC₅₀ of 0.1-1 μM, as well as ERK1/2 phosphorylation. In addition, Orantinib suppresses SCF-induced proliferation of MO7E cells with an IC₅₀ of 0.29 μM, and induces apoptosis^[2].

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

In Vivo

Orantinib (SU6668; 75-200 mg/kg) causes tumor growth inhibition on several tumor types in xenograft models in athymic mice, such as A375, Colo205, H460, Calu-6, C6, SF763T, and SKOV3TP5 cells. Orantinib (75 mg/kg) also inhibits tumor angiogenesis of C6 glioma xenografts^[1]. In a tumor model of HT29 human colon carcinoma, Orantinib (200 mg/kg) decreases the average vessel permeability and average fractional plasma volume in the tumor rim and core. Orantinib enhances abnormal stromal development at the periphery of carcinomas^[3]. Moreover, Orantinib (TSU-68; 200 mg/kg) augments the effect of chemotherapeutic infusion in a rabbit VX2 liver tumor model^[4].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 252916-29-3
Appearance Solid
Molecular Weight 310.35
Formula C₁₈H₁₈N₂O₃
Color Yellow to orange
SMILES

CC1=C(/C=C2C3=CC=CC=C3NC/2=O)NC(C)=C1CCC(O)=O
Synonyms

SU6668; TSU-68
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (6)

All

Sort by:

Journal Impact Factor

Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
J Control Release

Biomimetic nanocomplex based corneal neovascularization theranostics. [Abstract]

2024 Aug 9:374:50-60. PMID: 39111599
Cell Rep Methods

RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]

2023 Oct 23;3(10):100599. PMID: 37797618
J Pharm Sci

Construction of physiologically based pharmacokinetic model to predict CYP1A autoinduction by multi-kinase inhibitor TSU-68 based on in vitro induction kinetics. [Abstract]

2025 Aug 13;114(10):103953. PMID: 40816507
PLoS Genet

Juvenile hormone promotes paracellular transport of yolk proteins via remodeling zonula adherens at tricellular junctions in the follicular epithelium. [Abstract]

2022 Jun 27;18(6):e1010292. PMID: 35759519
Patent

US20180263995A1.

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (322.22 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.2222 mL

16.1108 mL

32.2217 mL

5 mM

0.6444 mL

3.2222 mL

6.4443 mL

10 mM

0.3222 mL

1.6111 mL

3.2222 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 10 mg/mL (32.22 mM); Clear solution

This protocol yields a clear solution of ≥ 10 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (100.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (805 KB)
- English - EN (805 KB)
- Français - FR (805 KB)
- Deutsch - DE (805 KB)
- Norwegian - NO (805 KB)
- Español - ES (805 KB)
- Swedish - SV (805 KB)
- Italian - IT (805 KB)
- Korean - KR (805 KB)
- Portuguese - PT (805 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Laird AD, et al. SU6668 is a potent antiangiogenic and antitumor agent that induces regression of established tumors. Cancer Res, 2000, 60(15), 4152-4160. [Content Brief]

[2]. Smolich BD, et al. The antiangiogenic protein kinase inhibitors SU5416 and SU6668 inhibit the SCF receptor (c-kit) in a human myeloid leukemia cell line and in acute myeloid leukemia blasts. Blood, 2001, 97(5), 1413-1421. [Content Brief]

[3]. Marzola P, et al. In vivo assessment of antiangiogenic activity of SU6668 in an experimental colon carcinoma model. Clin Cancer Res, 2004, 10(2), 739-750. [Content Brief]

[4]. Kim HC, et al. Augmentation of chemotherapeutic infusion effect by TSU-68, an oral targeted antiangiogenic agent, in a rabbit VX2 liver tumor model. Cardiovasc Intervent Radiol. 2012 Feb;35(1):168-75 [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.2222 mL	16.1108 mL	32.2217 mL	80.5542 mL
	5 mM	0.6444 mL	3.2222 mL	6.4443 mL	16.1108 mL
	10 mM	0.3222 mL	1.6111 mL	3.2222 mL	8.0554 mL
	15 mM	0.2148 mL	1.0741 mL	2.1481 mL	5.3703 mL
	20 mM	0.1611 mL	0.8055 mL	1.6111 mL	4.0277 mL
	25 mM	0.1289 mL	0.6444 mL	1.2889 mL	3.2222 mL
	30 mM	0.1074 mL	0.5370 mL	1.0741 mL	2.6851 mL
	40 mM	0.0806 mL	0.4028 mL	0.8055 mL	2.0139 mL
	50 mM	0.0644 mL	0.3222 mL	0.6444 mL	1.6111 mL
	60 mM	0.0537 mL	0.2685 mL	0.5370 mL	1.3426 mL
	80 mM	0.0403 mL	0.2014 mL	0.4028 mL	1.0069 mL
	100 mM	0.0322 mL	0.1611 mL	0.3222 mL	0.8055 mL

Keywords

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
Species:
Purity:
Quantity:

Orantinib

Anti-Infection Compound Library

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Covalent Screening Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Anti-COVID-19 Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cytokine Inhibitors Library

Cell Death Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Orantinib

All PDGFR Isoforms

All VEGFR Isoforms

Biological Activity

Chemical Information

Publications (6)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Orantinib Related Classifications

Cat. No.: HY-10517