上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。
SJG-136 (Synonyms: NSC-694501) 纯度: ≥98.0%
SJG-136 是一种有效的 DNA 交联剂 (DNA crosslinker),与 pBR322 DNA 交联的 XL50 值为 45 nM。SJG-136 具有抗肿瘤作用。
SJG-136 Chemical Structure
CAS No. : 232931-57-6
规格 | 价格 | 是否有货 | 数量 |
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10 mM * 1 mL in DMSO | ¥6000 | In-stock | |
1 mg | ¥2800 | In-stock | |
5 mg | ¥4900 | In-stock | |
10 mg | ¥7400 | In-stock | |
25 mg | ¥14800 | In-stock | |
50 mg | 询价 | ||
100 mg | 询价 |
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SJG-136 相关产品
•相关化合物库:
- Drug Repurposing Compound Library Plus
- Clinical Compound Library Plus
- Bioactive Compound Library Plus
- Toxins for Antibody-Drug Conjugate Research Library
生物活性 |
SJG-136 is a DNA cross-linking agent, with an XL50 of 45 nM for pBR322 DNA. SJG-136 has potent antitumor activity. |
IC50 & Target |
XL50: 45 nM (pBR322 DNA)[1] |
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体外研究 (In Vitro) |
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 45 nM for pBR322 DNA. SJG-136 is cytotoxic to ovarian cell lines, such as A2780 (IC50, 22.5 pM), A2780cisR (IC50, 24 pM), CH1 (IC50, 0.12 nM), CH1cisR (IC50, 0.6 nM), and SKOV-3 (IC50, 9.1 nM)[1]. SJG-136 (SG2000) also reduces the viability of a panel of canine cancer cells, with GI50 values ranging from 0.33 – >100 nM after a 1 h exposure, and <0.03 - 17.33 nM following continuous exposure[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (In Vivo) |
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[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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Clinical Trial |
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分子量 |
556.61 |
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Formula |
C31H32N4O6 |
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CAS 号 |
232931-57-6 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : 33.33 mg/mL (59.88 mM; Need ultrasonic) 配制储备液
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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。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
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参考文献 |
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Cell Assay [1] |
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 (160 μL) into 96-well microtiter plates and allowed to attach overnight. SJG-136 is dissolved in DMSO (to give a 20 mM concentration in each case) immediately prior to adding to the cells in quadruplicate wells. Final drug concentrations in the wells ranged from 100 μM to 2.5 nM as follows: 100, 25, 10, 2.5, 1 μM, and 250, 100, 25, 10, 2.5 nM. This is achieved by diluting the drugs in growth medium and then adding 40 μL 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 (100 μL of 10 mM) is added to each one. The plates are then shaken and absorbance readings taken at 540 nm 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[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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Animal Administration [2] |
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 (0.1 mL/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[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
参考文献 |
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