[CAS NO. 252916-29-3] Orantinib
PRODUCTS SPECIFICATIONS [252916-29-3]
DESCRIPTION [252916-29-3]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 310.35 |
| Molecular Formula | C18H18N2O3 |
| SMILES | CC1=C(/C=C2C3=CC=CC=C3NC/2=O)NC(C)=C1CCC(O)=O |
3 Publications Citing Use of MCE
Summary
IC50 & Target
|
PDGFRβ 8 nM (Ki) |
FGFR1 1.2 μM (Ki) |
Flt-1 2.1 μM (Ki) |
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 IC 50 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 IC 50 of 0.1-1 μM, as well as ERK1/2 phosphorylation. In addition, Orantinib suppresses SCF-induced proliferation of MO7E cells with an IC 50 of 0.29 μM, and induces apoptosis [2] .
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00024063 | Jonsson Comprehensive Cancer Center|National Cancer Institute (NCI) |
Breast Cancer|Colorectal Cancer|Gastric Cancer|Kidney Cancer|Lung Cancer|Multiple Myeloma and Plasma Cell Neoplasm|Pancreatic Cancer|Prostate Cancer
|
Phase 1 | |
| NCT01465464 | Taiho Pharmaceutical Co., Ltd. |
Hepatocellular Carcinoma
|
December 2010 | Phase 3 |
| NCT00784290 | Taiho Pharmaceutical Co., Ltd. |
Hepatocellular Carcinoma
|
September 2003 | Phase 1|Phase 2 |
| NCT00024206 | National Cancer Institute (NCI) |
Unspecified Adult Solid Tumor, Protocol Specific
|
July 2001 | Phase 1 |
Appearance
Solid
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
DMSO : ≥ 28 mg/mL ( 90.22 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 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 |
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1.
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.
- [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.
- [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.
- [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
Synonyms