BV6

目录号: GC12333纯度: >99.50%
A bivalent Smac mimetic and IAP antagonist

BV6
Cas No.: 1001600-56-1
规格价格库存数量操作
1mg¥317.00现货
1
2mg¥435.00现货
1
5mg¥585.00现货
1
10mg¥1,011.00现货
1
50mg¥3,002.00现货
1
10mM (in 1mL DMSO)¥1,341.00现货
1

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产品描述 Description

BV6 is a selective inhibitor of IAP family with IC50 value of 7.2 μM when tested with H460 cells [1].
IAP (inhibitor of apoptosis) is a family protein consists of 8 members and serves as endogenous inhibitors of programmed cell death. Until now, more than 5 human IAPs have been discovered includes XIAP, c-IAP1, c-IAP-2, NAIP, Livin and Survivin. It is reported that IAPs overexpression protects cells against a number of proapoptotic stimuli which enables IAPs play a pivotal role in promoting cancer cell survival [2, 3].
BV6 is an inhibitor of IAP family and often used as an adjuvant to sensitize the cancer cells to radiotherapy or chemotherapy. When tested with H460 NSCLC cells, pre-treatment BV6 sensitized the cells to radiation and increased the apoptosis in a time- and dose- dependent manner via reducing the expression of cIAP1 and XIAP [1]. In hematological THP-1 cells, pre-treatment with BV6 increased the CIK cells killing ability and the same results were achieved in solid malignancy RH30 cells [4]
In BALB/c mice model with transplanted abdominal cavities from donor mouse uterine tissue, intraperitoneally with BV6 repressed the advancement of endometriosis, cell proliferative activity via inhibiting the expression of IAPs [5].
References:
[1].    Li, W., et al., BV6, an IAP antagonist, activates apoptosis and enhances radiosensitization of non-small cell lung carcinoma in vitro. J Thorac Oncol, 2011. 6(11): p. 1801-9.
[2].    Altieri, D.C., Survivin - The inconvenient IAP. Semin Cell Dev Biol, 2015.
[3].    Fulda, S., Smac mimetics as IAP antagonists. Semin Cell Dev Biol, 2014.
[4].    Rettinger, E., et al., SMAC Mimetic BV6 Enables Sensitization of Resistant Tumor Cells but also Affects Cytokine-Induced Killer (CIK) Cells: A Potential Challenge for Combination Therapy. Front Pediatr, 2014. 2: p. 75.
[5].    Uegaki, T., et al., Inhibitor of apoptosis proteins (IAPs) may be effective therapeutic targets for treating endometriosis. Hum Reprod, 2015. 30(1): p. 149-58.

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

HCC193 and H460 non-small cell lung cancer (NSCLC) cell lines.

Preparation method

Limited solubility. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reaction Conditions

37℃

Applications

BV6 reduces the expression of cIAP1 and XIAP in HCC193 and H460 cell lines in a time and dose-dependent manner. BV6 also induces apoptosis in both HCC193 and H460 cell lines. In addition, BV6 prominently promotes the radiosensitivity of both HCC193 and H460 lung cancer cell lines.

Animal experiment [2]:

Animal models

Mouse endometriosis model

Dosage form

Single i.p. injection of BV6 (10 mg/kg) twice weekly.

Applications

BV6 treatment for 4 weeks attenuates the intensity of IAPs expression and lowers the total number of lesions, the average weight and the surface area of lesions as compared with control group. Moreover, BV6 treatment decreases the percentage of Ki67-positive cells in the endometrial gland epithelia or stroma.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

1. Li W, Li B, Giacalone NJ, Torossian A et al. BV6, an IAP antagonist, activates apoptosis and enhances radiosensitization of non-small cell lung carcinoma in vitro. J Thorac Oncol. 2011 Nov;6(11):1801-9.

2. Uegaki T, Taniguchi F, Nakamura K et al. Inhibitor of apoptosis proteins (IAPs) may be effective therapeutic targets for treating endometriosis. Hum Reprod. 2015 Jan;30(1):149-58.

产品文档 Product Documents

化学性质Chemical Properties

CAS 号
1001600-56-1
化学名
(S,S,2S,2'S)-N,N'-((2S,2'S)-(hexane-1,6-diylbis(azanediyl))bis(3-oxo-1,1-diphenylpropane-3,2-diyl))bis(1-((S)-2-cyclohexyl-2-((S)-2-(methylamino)propanamido)acetyl)pyrrolidine-2-carboxamide)
SMILES
O=C(CCCCCCCNC([C@@H](NC([C@H]1N(C([C@H](C2CCCCC2)NC([C@H](C)NC)=O)=O)CCC1)=O)CO=C(NCCCCCCNC([C@@H](NC([C@H]1N(C([C@H](C2CCCCC2)NC([C@H](C)NC)=O)=O)CCC1)=O)C(C3=CC=CC=C3)C4=CC=CC=C4)=O)[C@@H](NC([C@H]5N(C([C@H](C6CCCCC6)NC([C@H](C)NC)=O)=O)CCC5)=O)C(C7=CC=
分子式
C70H96N10O8
分子量
1205.57 g/mol
溶解性
≥ 60.2785mg/mL in DMSO
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
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°C,然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备 RT,或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol