Seviteronel (Synonyms: VT-464) |
| رقم الكتالوجGC37631 |
سيفيتيرونيل (VT-464) هو مثبط قوي للإنزيم CYP17 lyase (h-Lyase IC50 = 69 نانومتر) الذي أظهر اختيارية استثنائية في التحديد بالأشعة تحت الحمراء / المائية (~ 10 أضعاف) والنشاط الفموي في نموذج الهامستر لتثبيط توليد هرمونات الذكور.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1610537-15-9
Sample solution is provided at 25 µL, 10mM.
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Seviteronel (VT-464) is a potent CYP17 lyase inhibitor(h-Lyase IC50=69 nM) that demonstrated both exceptional in vitro lyase/hydroxylase selectivity (~10-fold) and oral activity in a hamster model of androgen biosynthesis inhibition. IC50: 69 nM(h-CYP17 Lyase)[1].
Seviteronel (VT-464), a non-steroidal small molecule inhibits androgen production without mineralocorticoid excess or cortisol depletion by selective inhibition of CYP17 17,20-lyase. We determined the impact of Seviteronel (VT-464) on tumor growth of a mCRPC xenograft, MDA-PCa-133, in vivo, and on androgen signaling in C4-2B prostate cancer cells in vitro[2].
The MDA-PCa-133 xenograft is derived from a clinical CRPC bone metastasis. Subcutaneous MDA-PCa-133 tumor expresses PSA, full-length androgen receptor (AR) and AR-V7 isoform. We determined the effect of Seviteronel (VT-464) and AA on MDA-PCa-133 growing in tumor-bearing castrated male mice: randomization into three groups; oral treatment with vehicle only, VT-464, (100 mg/kg bid), or AA (100 mg/kg bid) for 25 days. Both Seviteronel (VT-464) and AA reduced tumor volume (>two fold compared to vehicle; p<0.05). These results indicate that selective Seviteronel (VT-464) CYP17 lyase inhibition is as effective as AA CYP17 inhibition in this model [2].
[1]. Rafferty SW, et al. Highly-selective 4-(1,2,3-triazole)-based P450c17a 17,20-lyase inhibitors. Bioorg Med Chem Lett. 2014 Jun 1;24(11):2444-7. [2]. Sankar N. Maity, et al. Abstract 4772: Efficacy of VT-464, a novel selective inhibitor of cytochrome P450 17,20-lyase, in castrate-resistant prostate cancer models. Cancer Research: April 15, 2013; Volume 73, Issue 8, Supplement 1
| Cas No. | 1610537-15-9 | SDF | |
| المرادفات | VT-464 | ||
| Canonical SMILES | FC(F)OC1=C(OC(F)F)C=C(C=CC([C@](C2=CNN=N2)(C(C)C)O)=C3)C3=C1 | ||
| Formula | C18H17F4N3O3 | M.Wt | 399.34 |
| الذوبان | DMSO: ≥ 50 mg/mL (125.21 mM) | 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5041 mL | 12.5207 mL | 25.0413 mL |
| 5 mM | 0.5008 mL | 2.5041 mL | 5.0083 mL |
| 10 mM | 0.2504 mL | 1.2521 mL | 2.5041 mL |
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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.
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Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 7 reference(s) in Google Scholar.)
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