| Size | Price | |
|---|---|---|
| 100mg | ||
| 500mg |
| ln Vitro |
Flk-1 trans-phosphorylation (Ki=2.1 μM), FGFR1 trans-phosphorylation (Ki=1.2 μM), and PDGFR autophosphorylation (Ki=0.008 μM) are all inhibited by SU6668 (5–15 minutes) [1]. In HUVEC, the VEGF-stimulated rise in KDR tyrosine phosphorylation is inhibited by SU6668 (0.03-10 μM; 60 minutes) [1]. With an IC50 of 0.34 and 9.6 μM, respectively, SU6668 suppresses VEGF- and FGF-induced HUVEC mitosis in a dose-dependent manner [1].
|
|---|---|
| ln Vivo |
SU6668 (4-200 mg/kg/day; orally for 21 days) promotes dose-dependent suppression of A431 tumor growth in athymic mice [1]. SU6668 (75 mg/kg/day; intraperitoneally injected for 22 days) effectively reduces tumor angiogenesis and vascularization in mice [1]. SU6668 (200 mg/kg/day; orally for 11-27 days) induces considerable regression of established big A431 xenografts in athymic mice [1].
|
| Animal Protocol |
Animal/Disease Models: Female athymic mice (BALB/c, nu/nu) implanted with A431 tumor cells [1]
Doses: 4, 40, 75, 200 mg/kg Route of Administration: Oral daily for 21 days Experimental Results: Induction 97% growth inhibition of A431 tumors at dose 97%. No deaths were observed in any treatment group. |
| ADME/Pharmacokinetics |
Metabolism / Metabolites
TSU-68 has known human metabolites that include TSU-68 metabolite 1, TSU-68 metabolite 2, and TSU-68 metabolite 3. |
| References |
|
| Additional Infomation |
Orantinib has been used in trials studying the treatment of Lung Cancer, Breast Cancer, Kidney Cancer, Gastric Cancer, and Prostate Cancer, among others.
Orantinib is an orally bioavailable receptor tyrosine kinase inhibitor. SU6668 binds to and inhibits the autophosphorylation of vascular endothelial growth factor receptor 2 (VEGFR2), platelet-derived growth factor receptor (PDGFR), and fibroblast growth factor receptor (FGFR), thereby inhibiting angiogenesis and cell proliferation. SU6668 also inhibits the phosphorylation of the stem cell factor receptor tyrosine kinase c-kit, often expressed in acute myelogenous leukemia cells. (NCI04) |
| Molecular Formula |
C18H18N2O3
|
|---|---|
| Molecular Weight |
310.347
|
| Exact Mass |
310.131
|
| CAS # |
210644-62-5
|
| Related CAS # |
Orantinib;252916-29-3
|
| PubChem CID |
5329099
|
| Appearance |
Orange to red solid powder
|
| Density |
1.3±0.1 g/cm3
|
| Boiling Point |
590.5±50.0 °C at 760 mmHg
|
| Flash Point |
310.9±30.1 °C
|
| Vapour Pressure |
0.0±1.7 mmHg at 25°C
|
| Index of Refraction |
1.675
|
| LogP |
2.49
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
23
|
| Complexity |
516
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC1=C(NC(=C1CCC(=O)O)C)/C=C\2/C3=CC=CC=C3NC2=O
|
| InChi Key |
NHFDRBXTEDBWCZ-ZROIWOOFSA-N
|
| InChi Code |
InChI=1S/C18H18N2O3/c1-10-12(7-8-17(21)22)11(2)19-16(10)9-14-13-5-3-4-6-15(13)20-18(14)23/h3-6,9,19H,7-8H2,1-2H3,(H,20,23)(H,21,22)/b14-9-
|
| Chemical Name |
3-[2,4-dimethyl-5-[(Z)-(2-oxo-1H-indol-3-ylidene)methyl]-1H-pyrrol-3-yl]propanoic acid
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~161.11 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (6.70 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.08 mg/mL (6.70 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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