Shopping Cart
  • Remove All
  • TargetMol
    Your shopping cart is currently empty

Orantinib

Catalog No. T6184Cas No. 252916-29-3
Alias TSU-68, SU6668, NSC 702827

Orantinib (NSC 702827) , a excellent effective against PDGFR autophosphorylation with Ki of 8 nM, also highly inhibits Flk-1 and FGFR1 trans-phosphorylation. It shows little effect against IGF-1R, Met, Src, Lck, Zap70, Abl and CDK2 and does not suppresses EGFR.

Orantinib

Orantinib

Purity: 100%
Catalog No. T6184Alias TSU-68, SU6668, NSC 702827Cas No. 252916-29-3
Orantinib (NSC 702827) , a excellent effective against PDGFR autophosphorylation with Ki of 8 nM, also highly inhibits Flk-1 and FGFR1 trans-phosphorylation. It shows little effect against IGF-1R, Met, Src, Lck, Zap70, Abl and CDK2 and does not suppresses EGFR.
Pack SizePriceAvailabilityQuantity
5 mg$47In Stock
10 mg$72In Stock
25 mg$153In Stock
50 mg$293In Stock
100 mg$515In Stock
1 mL x 10 mM (in DMSO)$51In Stock
Bulk & Custom
Add to Cart
Questions
View More

Related Compound Libraries of "Orantinib"

Select Batch
Purity:100%
Contact us for more batch information
Resource Download
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.

Product Introduction

Bioactivity
Description
Orantinib (NSC 702827) , a excellent effective against PDGFR autophosphorylation with Ki of 8 nM, also highly inhibits Flk-1 and FGFR1 trans-phosphorylation. It shows little effect against IGF-1R, Met, Src, Lck, Zap70, Abl and CDK2 and does not suppresses EGFR.
Targets&IC50
PDGFRβ:8 nM(Ki)
In vitro
In the HT29 human colorectal cancer tumor model, TSU-68 (200 mg/kg) reduced the average vascular permeability at the tumor margin and the average plasma volume fraction at the tumor center. In athymic mice bearing various xenografts, including A375, Colo205, H460, Calu-6, C6, SF763T, and SKOV3TP5 cells, TSU-68 (75-200 mg/kg) inhibited cell growth. In the rabbit VX2 liver tumor model, TSU-68 (200 mg/kg) enhanced the efficacy of injected chemotherapy. Additionally, in C6 glioma xenografts, TSU-68 (75 mg/kg) also blocked tumor angiogenesis.
In vivo
TSU-68 is an ATP-competitive inhibitor that acts on Flk-1/KDR, FGFR1, and PDGFRβ kinase phosphorylation with respective Ki values of 2.1 μM, 1.2 μM, and 8 nM. In human megakaryoblastic leukemia MO7E cells, TSU-68 (IC50=0.1-1 μM) inhibits the tyrosine autophosphorylation of the c-kit receptor for hepatocyte growth factor and the phosphorylation of ERK1/2. It also suppresses cell proliferation and induces apoptosis in MO7E cells stimulated by SCF, with an IC50 of 0.29 μM. In NIH-3T3 cells overexpressing PDGFRβ, TSU-68 (0.03-0.1 μM) inhibits the PDGFRβ tyrosine phosphorylation stimulated by PDGF. Additionally, in human umbilical vein endothelial cells (HUVECs) stimulated by vascular endothelial growth factor, TSU-68 (0.03-10 μM) prevents KDR tyrosine phosphorylation. However, in NIH-3T3 cells overexpressing EGFR, TSU-68 (100 μM) does not inhibit the tyrosine phosphorylation of EGFR stimulated by EGF. Furthermore, TSU-68 inhibits the proliferation of HUVECs driven by vascular endothelial growth factor and FGF, with average IC50 values of 0.34 and 9.6 μM, respectively.
Kinase Assay
trans-Phosphorylation Reactions: Tyrosine kinase assays to quantitate the trans-phosphorylation activity of Flk-1 and FGFR1 are performed in 96-well microtiter plates precoated (20 μg/well in PBS; incubated overnight at 4 °C) with the peptide substrate poly-Glu,Tyr (4:1). Excess protein binding sites are blocked with 1-5% (w/v) BSA in PBS. Purified GST-FGFR1 (kinase domain) or GST-Flk-1 (cytoplasmic domain) fusion proteins are then added to the microtiter wells in 2 × concentration kinase dilution buffer consisting of 100 mM HEPES, 50 mM NaCl, 40 μM NaVO4, and 0.02% (w/v) BSA. The final enzyme concentration for GST-Flk-1 and GST-FGFR1 is 50 ng/mL. SU6668 is dissolved in DMSO at 100× the final required concentration and diluted 1:25 in Water. Twenty-five μL of diluted SU6668 are subsequently added to each reaction well. The kinase reaction is initiated by the addition of different concentrations of ATP in a solution of MnCl2 so that the final ATP concentrations spanned the Km for the enzyme, and the final concentration of MnCl2 is 10 mM. The plates are incubated for 5-15 min at room temperature before stopping the reaction with the addition of EDTA. The plates are then washed three times with TBST. Rabbit polyclonal antiphosphotyrosine antisera are added to the wells at a 1: 10000 dilution in TBST containing 0.5% (w/v) BSA, 0.025% (w/v) nonfat dry milk, and 100 μM NaVO4 and incubated for 1 hour at 37 °C. The plates are then washed three times with TBST, followed by the addition of goat anti-rabbit antisera conjugated with HRP. The plates are incubated for 1 hour at 37 °C and then washed three times with TBST. The amount of phosphotyrosine in each well is quantitated after the addition of 2,2
Cell Research
Cells are seeded (3 × 105 cells/35-mm well) in DMEM containing 10% (v/v) FBS and grow to confluence and then quiesced in DMEM containing 0.1% serum for 2 hours before drug treatment. HUVECs (seeded at 2 × 106 cells/10-cm plate) are grown to confluence in endothelial cell growth media and then quiesced in endothelial cell basal media containing 0.5% FBS for 24 hours before drug treatment. All cell lines are incubated with SU6668 for 1 hour before ligand stimulation (100 ng/mL) for 10 min. Western blotting is perfor (Only for Reference)
AliasTSU-68, SU6668, NSC 702827
Chemical Properties
Molecular Weight310.35
FormulaC18H18N2O3
Cas No.252916-29-3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
1eq. NaOH: 31 mg/mL (100 mM)
DMSO: 40 mg/mL (128.89 mM), Sonication is recommended.
Solution Preparation Table
1eq. NaOH/DMSO
1mg5mg10mg50mg
1 mM3.2222 mL16.1108 mL32.2217 mL161.1084 mL
5 mM0.6444 mL3.2222 mL6.4443 mL32.2217 mL
10 mM0.3222 mL1.6111 mL3.2222 mL16.1108 mL
20 mM0.1611 mL0.8055 mL1.6111 mL8.0554 mL
50 mM0.0644 mL0.3222 mL0.6444 mL3.2222 mL
100 mM0.0322 mL0.1611 mL0.3222 mL1.6111 mL

Calculator

  • Molarity Calculator
  • Dilution Calculator
  • Reconstitution Calculator
  • Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
%Tween 80
%ddH2O

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

Keywords

Related Tags: buy Orantinib | purchase Orantinib | Orantinib cost | order Orantinib | Orantinib chemical structure | Orantinib in vivo | Orantinib in vitro | Orantinib formula | Orantinib molecular weight