(Z)-Orantinib
Based on 1 Customer Validation
(Z)-Orantinib ((Z)-SU6668) is a potent, selective, orally active and ATP competitive inhibitor of Flk‐1/KDR, PDGFRβ, and FGFR1, with IC50s of 2.1, 0.008, and 1.2 µM, respectively. (Z)-Orantinib is a potent antiangiogenic and antitumor agent that induces regression of established tumors.
For research use only. We do not sell to patients.
- Purity: 99.44%
- CAS No.: 210644-62-5
- Formula: C18H18N2O3
- Molecular Weight:310.35
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
All VEGFR Isoforms
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Biological Activity
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Flk-1/KDR 2.1 μM (IC50) |
PDGFRβ 0.008 μM (IC50) |
FGFR1 1.2 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 3T3 | IC50 |
1 μM
Compound: 5b
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Inhibition of Platelet-derived growth factor induced 3T3 cell proliferation
Inhibition of Platelet-derived growth factor induced 3T3 cell proliferation
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[PMID: 12646019] |
| HUVEC | IC50 |
>50 μM
Compound: SU-6668
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Inhibition of rhFGF2-induced cellular proliferation of HUVEC
Inhibition of rhFGF2-induced cellular proliferation of HUVEC
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[PMID: 17618113] |
| HUVEC | IC50 |
>50 μM
Compound: SU-6668
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Inhibition of rhFGF2-induced HUVEC proliferation
Inhibition of rhFGF2-induced HUVEC proliferation
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[PMID: 19110422] |
| HUVEC | IC50 |
3.9 μM
Compound: 51
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Inhibition of VEGFR2 phosphorylation in HUVEC by chemiluminescence assay
Inhibition of VEGFR2 phosphorylation in HUVEC by chemiluminescence assay
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[PMID: 20403700] |
| MV4-11 | IC50 |
3.9 μM
Compound: Orantinib
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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
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[PMID: 29935772] |
| NIH3T3 | IC50 |
0.1 μM
Compound: 51
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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
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[PMID: 20403700] |
| NIH3T3 | IC50 |
0.3 μM
Compound: 5b
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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
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[PMID: 12646019] |
| NIH3T3 | IC50 |
16 μM
Compound: 5b
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Inhibition of PDGF-induced BrdU incorporation in 3T3 cells
Inhibition of PDGF-induced BrdU incorporation in 3T3 cells
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[PMID: 12646019] |
| NIH3T3 | IC50 |
2 μM
Compound: 5b
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Inhibition of Vascular endothelial growth factor receptor in 3T3 cells
Inhibition of Vascular endothelial growth factor receptor in 3T3 cells
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[PMID: 12646019] |
| NIH3T3 | IC50 |
36 μM
Compound: 5b
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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
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[PMID: 12646019] |
| NIH3T3 | IC50 |
49 μM
Compound: 5b
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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
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[PMID: 12646019] |
| NIH3T3 | IC50 |
9.5 μM
Compound: 5b
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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
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[PMID: 12646019] |
| Sf9 | IC50 |
28.4 μM
Compound: R2C3, 30
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Inhibition of human GST-fused ZAP-70 expressed in Sf9 cells
Inhibition of human GST-fused ZAP-70 expressed in Sf9 cells
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[PMID: 19674816] |
SU6668 (5-15 min) inhibits Flk-1 trans-phosphorylation (Ki=2.1 μM), FGFR1 trans-phosphorylation (Ki=1.2 μM), and PDGFR autophosphorylation (Ki=0.008 μM)[1].
SU6668 (0.03-10 μM; 60 min) inhibits the VEGF-stimulated increase of KDR tyrosine phosphorylation in HUVECs[1].
SU6668 inhibits mitogenesis of HUVECs induced by both VEGF and FGF in a dose-dependent manner with IC50s of 0.34 and 9.6 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
SU6668 (75 mg/kg/day; i.p. for 22 d) significantly suppresses tumor angiogenesis and vascularization in mice[1].
SU6668 (200 mg/kg/day; p.o. for 11-27 d) induces striking regression of large established A431 xenografts in athymic mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female athymic mice (BALB/c, nu/nu) were implanted A431 tumor cells[1]
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Dosage:4, 40, 75, 200 mg/kg
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Administration:P.o. daily for 21 days
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Result:Induced 97% growth inhibition against A431 tumor at the dose of 97%.
No mortality was observed in any treatment group.
Chemical Information
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CAS No. 210644-62-5
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Appearance Solid
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Molecular Weight 310.35
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Formula C18H18N2O3
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Color Orange to red
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SMILES
O=C(O)CCC1=C(C)NC(/C=C2C(NC3=C\2C=CC=C3)=O)=C1C.[(Z)]
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Synonyms
(Z)-SU6668; (Z)-TSU-68
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 50 mg/mL (161.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.08 mg/mL (6.70 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (6.70 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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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 Aug 1;60(15):4152-60. [Content Brief]
[2]. Laird ad, et, al. SU6668 inhibits Flk-1/KDR and PDGFRbeta in vivo, resulting in rapid apoptosis of tumor vasculature and tumor regression in mice. FASEB J. 2002 May;16(7):681-90. [Content Brief]
Complete Stock Solution Preparation Table
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| 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 |
(Z)-Orantinib Related Classifications
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