(Z)-Orantinib (Synonyms: (Z)-SU6668; (Z)-TSU-68) |
| رقم الكتالوجGC62291 |
(Z) -Orantinib ((Z) -SU6668) هو مثبط فعال وانتقائي وفعال عن طريق الفم ومانع ATP تنافسي لـ Flk ‐ 1 / KDR و PDGFRβ و FGFR1 ، مع IC50s من 2.1 ، 0.008 ، و 1.2 ميكرومتر ، على التوالي(Z) -Orantinib هو عامل مضاد لتكوُّن الأوعية الدموية ومضاد للأورام يؤدي إلى تراجع الأورام المستقرة
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Cas No.: 210644-62-5
Sample solution is provided at 25 µL, 10mM.
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(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[1][2].
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].
SU6668 (4-200 mg/kg/day; p.o. for 21 d) induces dose-dependent inhibition of A431 tumor growth in athymic mice[1].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].
[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.
[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.
| Cas No. | 210644-62-5 | SDF | |
| المرادفات | (Z)-SU6668; (Z)-TSU-68 | ||
| Formula | C18H18N2O3 | M.Wt | 310.35 |
| الذوبان | DMSO : 50 mg/mL (161.11 mM; Need ultrasonic) | 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. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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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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
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 38 reference(s) in Google Scholar.)
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