Orantinib
Based on 6 publication(s) in Google Scholar
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.52%
- CAS 番号: 252916-29-3
- 分子式: C18H18N2O3
- 分子量:310.35
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 Orantinib
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生物活性
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PDGFRβ 8 nM (Ki) |
FGFR1 1.2 μM (Ki) |
Flt-1 2.1 μM (Ki) |
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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 |
16 μM
Compound: 5b
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Inhibition of PDGF-induced BrdU incorporation in 3T3 cells with 0.5% bovine serum albumin
Inhibition of PDGF-induced BrdU incorporation in 3T3 cells with 0.5% bovine serum albumin
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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] |
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 IC50 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 IC50 of 0.1-1 μM, as well as ERK1/2 phosphorylation. In addition, Orantinib suppresses SCF-induced proliferation of MO7E cells with an IC50 of 0.29 μM, and induces apoptosis[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 252916-29-3
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性状 Solid
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分子量 310.35
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分子式 C18H18N2O3
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Color Yellow to orange
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SMILES
CC1=C(/C=C2C3=CC=CC=C3NC/2=O)NC(C)=C1CCC(O)=O
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別名
SU6668; TSU-68
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (6)
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Journal Impact Factor
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Most Recent
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Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
J Control Release
2024 Aug 9:374:50-60. PMID: 39111599 -
Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618 -
J Pharm Sci
Construction of physiologically based pharmacokinetic model to predict CYP1A autoinduction by multi-kinase inhibitor TSU-68 based on in vitro induction kinetics. [Abstract]2025 Aug 13;114(10):103953. PMID: 40816507 -
PLoS Genet
Juvenile hormone promotes paracellular transport of yolk proteins via remodeling zonula adherens at tricellular junctions in the follicular epithelium. [Abstract]2022 Jun 27;18(6):e1010292. PMID: 35759519 -
溶剤 & 溶解度
DMSO : 100 mg/mL (322.22 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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: ≥ 10 mg/mL (32.22 mM); Clear solution
This protocol yields a clear solution of ≥ 10 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (100.0 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.
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.
純度とドキュメンテーション
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データシート (277 KB)
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SDS (805 KB)
- English - EN (805 KB)
- Français - FR (805 KB)
- Deutsch - DE (805 KB)
- Norwegian - NO (805 KB)
- Español - ES (805 KB)
- Swedish - SV (805 KB)
- Italian - IT (805 KB)
- Korean - KR (805 KB)
- Portuguese - PT (805 KB)
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取扱説明書 (2659 KB)
参考文献
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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 [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| 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 |
Orantinib 関連分類
HY-10517 関連分類
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