SV119
SV119 is a selective sigma-2 (σ₂) receptor ligand (Ki ≈ 5-10 nM). SV119 induces apoptosis in various human cancer cell lines by activating caspase-3 and promoting mitochondrial depolarization. SV119 can enhance the effects of chemotherapeutic agents such as Paclitaxel (HY-B0015), increasing their cytotoxicity against tumor cells. SV119 significantly inhibits tumor growth in mouse xenograft models, both alone and in combination. SV119 is useful in the research of cancers such as breast, prostate, and pancreatic cancer.
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- CAS No.: 913815-82-4
- 화학식: C23H37N3O3
- 분자량:403.56
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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Caspase 3 |
Caspase-7 |
SV119 (0-10 µM) induces caspase-3/7 dependent apoptosis against Panc1, CFPAC, ASPC, PancO2 cells[1].
SV119 has an EC50 of 23.3 μM in MDA-MB-231 cells (100% maximal cytotoxicity) and 17.6 μM in MCF-7 cells (100 % maximal cytotoxicity) for sigma-2 receptor[2].
SV119 (30 µM, 24-48 h) decreases protein levels of full-length Bid[2].
SV119 (0-10 µM, 24 h) increases apoptosis in ASPC-1, CFPAC, Panc1, PancO2 cells in combination with Gemcitabine (HY-17026) and Paclitaxel (HY-B0015)[4].
SV119 (10 mM, 1.5 h) reduces the fluorescence of cancer stem cell (CSC) in MDA-MB-435 cells[5].
SV119 (SV119-PEG-AuNC/DOX, cover density (50%)) significantly reduces the formation and number of mammary cells and decreases the stemness of breast CSCs in combination with photothermal and chemotherapy in MDA-MB-435 cells[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Panc02 cells
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Concentration:0, 10 µM
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Incubation Time:24 h
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Result:Induced apoptosis in cells that were both in G0 as well as in G1 to G2/S phase of the cell cycle in combination with Gemcitabine and Paclitaxel, with mean TUNEL-positivity ranged from 16.1% to 18.6% at 10 μM.
Increased mean TUNEL-positivity ranged from 26.5% to 70.5% in gemcitabine combination (50 nM) and from 26.6% to 53.8% in paclitaxel combination (50 nM).
Induced moderate apoptosis in Ki67 negative cells (G0 phase).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Panc-02 (106) pancreatic tumors C57BL/6 mice (8-12 weeks old) model[4]
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Dosage:1 mg/mouse
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Administration:i.p., once
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Result:Increased apoptosis that were treated with conventional chemotherapy (Gemcitabine or Paclitaxel).
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Animal Model:Panc-02 (106) pancreatic tumors C57BL/6 mice (8-12 weeks old) model[4]
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Dosage:1 mg/mouse and weekly gemcitabine (3 mg/mouse, i.p. for two weeks)/daily paclitaxel (0.3 mg/mouse, i.p. for 7 days)
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Administration:i.p. every other day/daily, for 7 days
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Result:Demonstrated a non significant tumor volume and survival advantage, significantly slowed tumor growth in combination with Gemcitabine and Paclitaxel.
Chemical Information
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CAS No. 913815-82-4
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분자량 403.56
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화학식 C23H37N3O3
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SMILES
NCCCCCCN([C@@]1([H])C2)[C@](CCC1)([H])C[C@H]2OC(NC(C=C3C)=C(C=C3)OC)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[1]. Kashiwagi H, et al. Selective sigma-2 ligands preferentially bind to pancreatic adenocarcinomas: applications in diagnostic imaging and therapy. Mol Cancer. 2007 Jul 15;6:48. [Content Brief]
[4]. Kashiwagi H, et al. Sigma-2 receptor ligands potentiate conventional chemotherapies and improve survival in models of pancreatic adenocarcinoma. J Transl Med. 2009 Mar 26;7:24. [Content Brief]
[5]. Sun T, et al. Using SV119-gold nanocage conjugates to eradicate cancer stem cells through a combination of photothermal and chemo therapies. Adv Healthc Mater. 2014 Aug;3(8):1283-91. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SV119 Related Classifications
HY-177345 Related Classifications
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