TSU-68 (SU6668,Orantinib) (Synonyms: NSC 702827, Orantinib, TSU68) |
| Catalog No.GC16732 |
TSU-68 (SU6668,Orantinib) (SU6668; TSU-68) is a multi-targeted receptor tyrosine kinase inhibitor with Kis of 2.1 μM, 8 nM and 1.2 μM for Flt-1, PDGFRβ and FGFR1, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 252916-29-3
Sample solution is provided at 25 µL, 10mM.
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Ki: Flk-1trans-phosphorylation (2.1 mM), FGFR1 trans-phosphorylation (1.2 mM), and PDGFR autophosphorylation (0.008 mM).
Vascular endothelial growth factor, fibroblast growth factor (FGF), and platelet-derived growth factor (PDGF) and their cognate receptor tyrosine kinases are strongly implicated in angiogenesis associated with solid tumors. TSU-68 is a novel inhibitor of these receptors.
In vitro: Biochemical kinetic studies using isolated Flk-1, FGF receptor 1, and PDGF receptor β kinases revealed that TSU-68 has competitive inhibitory properties with respect to ATP. In cellular systems, TSU-68 inhibited receptor tyrosine phosphorylation and mitogenesis after stimulation of cells by appropriate ligands [1].
In vivo: Oral or i.p. administration of TSU-68 in athymic mice resulted in significant growth inhibition of a diverse panel of human tumor xenografts of glioma, melanoma, lung, colon, ovarian, and epidermoid origin [1].
Clinical trial: Phase I clinical study indicated that TSU-68 can be safely combined with standard doses of carboplatin-paclitaxel, with the combination manifesting promising antitumor activity [2].
References:
[1] Laird AD, Vajkoczy P, Shawver LK et al. SU6668 is a potent antiangiogenic and antitumor agent that induces regression of established tumors. Cancer Res. 2000 Aug 1;60(15):4152-60.
[2] Okamoto I, Yoshioka H, Takeda K et al. Phase I clinical study of the angiogenesis inhibitor TSU-68 combined with carboplatin and paclitaxel in chemotherapy-naive patients with advanced non-small cell lung cancer. J Thorac Oncol. 2012 Feb;7(2):427-33.
| Cas No. | 252916-29-3 | SDF | |
| Synonyms | NSC 702827, Orantinib, TSU68 | ||
| Chemical Name | 3-[2,4-dimethyl-5-[(Z)-(2-oxo-1H-indol-3-ylidene)methyl]-1H-pyrrol-3-yl]propanoic acid | ||
| Canonical SMILES | CC1=C(NC(=C1CCC(=O)O)C)C=C2C3=CC=CC=C3NC2=O | ||
| Formula | C18H18N2O3 | M.Wt | 310.35 |
| Solubility | ≥ 15.5mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 31 reference(s) in Google Scholar.)
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