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SJG-136  ≥95%

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包装规格：2mg 5mg 10mg 25mg in glass bottle
溶解性：溶于DMSO（33.33 mg/mL 超声）
产品描述：基本信息 产品编号： S10651 产品名称： SJG-136 CAS: 232931-57-6   储存条件 粉末 -20℃ 四年     分子式： C31H32N4O6 溶于液体 -80℃ 6个月 分子量 556.61 -20℃ 1个月 化学名：  (6aS)-3-[3-[[(6aS)-2-methoxy-8-methylidene-11-oxo-7,9-dihydro-6aH-pyrrolo[2,1-c][1,4]benzodiazepin-3-yl]oxy]propoxy]-2-methoxy-8-methylidene-7,9-dihydro-6aH-pyrrolo[2,1-c][1,4]benzodiazepin-11-one Solubility (25°C)：   体外:   DMSO 30mg/mL (53.90mM; Need ultrasonic) Water   Ethanol   体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 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。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 1.7966mL 8.9830mL 17.9659mL 5mM 0.3593mL 1.7966mL 3.5932mL 10mM 0.1797mL 0.8983mL 1.7966mL   生物活性 产品描述 一种有效的 DNA 交联剂，与 pBR322 DNA 交联的 XL50 值为 45nM。 靶点 XL50: 45nM (pBR322 DNA) 体外研究 SJG-136 (dimer 5) is a DNA cross-linking agent, with an XL50 (concentration of agent required for 50% cross-linking of pBR322 DNA) of 45nM for pBR322 DNA. SJG-136 is cytotoxic to ovarian cell lines, such as A2780 (IC50, 22.5pM), A2780cisR (IC 50, 24pM), CH1 (IC50, 0.12nM), CH1cisR (IC50, 0.6nM), and SKOV-3 (IC50, 9.1nM). SJG-136 (SG2000) also reduces the viability of a panel of canine cancer cells, with GI50 values ranging from 0.33 - >100nM after a 1 h exposure, and 体内研究 SJG-136 shows more potent antitumor effect against CMeC-1 tumour at 0.30 mg/kg than 0.15 mg/kg either as a single dose or administered once a week for three weeks via dosed intravenously in mice. SJG-136-induced H2AX phosphorylation shows good correspondence, but less sensitivity, than measurement of foci 特征     推荐实验方法(仅供参考) Cell Assay In vitro cytotoxicity is evaluated using the human ovarian carcinoma cell lines SKOV-3, A2780, and CH1, together with the cisplatin-resistant counterparts of the A2780 and CH1 lines (A2780cisR and CH1cisR, respectively). Viable cells are seeded in growth medium (160μL) into 96-well microtiter plates and allowed to attach overnight. SJG-136 is dissolved in DMSO (to give a 20mM concentration in each case) immediately prior to adding to the cells in quadruplicate wells. Final drug concentrations in the wells ranged from 100μM to 2.5nM as follows: 100, 25, 10, 2.5, 1μM, and 250, 100, 25, 10, 2.5nM. This is achieved by diluting the drugs in growth medium and then adding 40μL to the existing well volume of 160 μL to give the final concentrations stated above. After 4 days (96 h), the medium is removed and the remaining cells are fixed using 10% trichloroacetic acid on ice for 30 min. Wells are then washed 3−4 times with tap water and air-dried overnight, and 100 μL of 0.4% sulforhodamine B (dissolved in 1% glacial HOAc) is added to each well. Staining is allowed to continue for 10−15 min; the wells are then washed 3−4 times with 1% acetic acid and air-dried, and Tris base (100μL of 10mM) is added to each one. The plates are then shaken and absorbance readings taken at 540nm using a plate reader. From plots of concentration versus percentage absorbance (compared to 8 untreated wells), IC50 values are calculated using the Quattro-Pro software package   Animal Administration A homogenous suspension of 5 × 106 exponentially growing canine melanoma cells in serum free RPMI 1640 tissue culture medium is injected subcutaneously into CD1 Nu/Nu immunocompromised female mice. The mice are divided into five groups of ten mice, with equivalent mean tumour volumes for each group. SJG-136 is given intravenously into the tail vein to four of these groups and vehicle control is administered to the fifth group. SJG-136 injections are prepared in 0.9 % NaCl and 1 % DMSO vehicle. Animals are weighed prior to the injection to determine the volume of SJG-136 required (0.1mL/10 g body weight) which is given IV in the tail vein. Control group mice are given an IV injection of the vehicle solution; mice in groups one and two are given a single treatment of SJG-136, 0.15 mg/kg and 0.30 mg/kg respectively; mice in groups four and five are given 0.15 mg/kg and 0.30 mg/kg respectively, every seven days for a total of three treatments
保存条件：-20℃

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