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VR23 Sale

目录号 : GC12003

A proteasome inhibitor

VR23 Chemical Structure

Cas No.:1624602-30-7

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥545.00
现货
5mg
¥495.00
现货
10mg
¥855.00
现货
50mg
¥2,880.00
现货
100mg
¥4,950.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

VR23 is an effective proteasome inhibitor, with IC50 values of 3 μmol/L, 1 nmol/L, and 50-100 nmol/L to inhibit activities of caspase-like proteasomes, trypsin-like proteasomes, and chymotrypsin-like proteasomes, respectively [1].

As a regulator, the ubiquitin-proteasome system is important for cell growth and apoptosis [2]. The ubiquitin-proteasome pathway is critical in the regulated degradation of proteins involved in tumor growth and cell cycle control [3].

Treatment with VR23 made cancer cells undergo an abnormal centrosome amplification cycle. This cycle was caused by the accumulation of ubiquitinated cyclin E. Bortezomib is clinically approved as a chymotrypsin-like proteasome inhibitor. VR23 in combinations with bortezomib, caused a synergistic effect in killing multiple myeloma cells. This synergistic effect was also effective to myeloma cells resistant to bortezomib [1].

In vivo, VR23 was effective in controlling metastatic breast cancer cells and multiple myelomas [1]. In engrafted animals, the treatment with VR23 at 30 mg/kg twice per week for three weeks inhibited tumor growth effectively. Following 24 hours pre-treatment with paclitaxel at 20mg/kg/week, the administration of VR23 enhanced the anti-tumor activity of paclitaxel by 70%. Histological data showed that VR23 substantially decreased mitotic index, inhibited tumor infiltration into surrounding tissues and remarkably reduced tumor cell proliferation and angiogenesis [4].

References:
[1].  Pundir S, Vu HY, Solomon VR, et al. VR23: A Quinoline-Sulfonyl Hybrid Proteasome Inhibitor That Selectively Kills Cancer via Cyclin E-Mediated Centrosome Amplification. Cancer research, 2015, 75(19): 4164-4175.
[2].  Almond JB, Cohen GM. The proteasome: a novel target for cancer chemotherapy. Leukemia, 2002, 16(4): 433-443.
[3].  Adams J, Palombella VJ, Sausville EA, et al. Proteasome inhibitors: a novel class of potent and effective antitumor agents. Cancer research, 1999, 59(11): 2615-2622.
[4].  Vu HYT, Pundir S, Solomon RV, et al. Anticancer effects and mechanism of VR23, a novel chloroquine derivative. Cancer Research, 2014, 74(19 Supplement): 4545-4545.

Chemical Properties

Cas No. 1624602-30-7 SDF
化学名 7-chloro-4-(4-((2,4-dinitrophenyl)sulfonyl)piperazin-1-yl)quinoline
Canonical SMILES ClC1=CC2=C(C(N3CCN(S(C4=C([N+]([O-])=O)C=C([N+]([O-])=O)C=C4)(=O)=O)CC3)=CC=N2)C=C1
分子式 C19H16ClN5O6S 分子量 477.88
溶解度 ≥ 45.55mg/mL in DMSO 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.0926 mL 10.4629 mL 20.9258 mL
5 mM 0.4185 mL 2.0926 mL 4.1852 mL
10 mM 0.2093 mL 1.0463 mL 2.0926 mL
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