Namitecan (ST-1968)
(Synonyms: ST-1968) 目录号 : GC34156
Namitecan (ST-1968) 是一种有效的拓扑异构酶 I 抑制剂，具有抗肿瘤特性。
Cas No.:372105-27-6
Sample solution is provided at 25 µL, 10mM.
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Namitecan is a potent topoisomerase I inhibitor, with antitumor property.
Namitecan and cetuximab cooperate in inhibiting EGFR expression. Namitecan induces a dose-dependent decrease in EGFR expression in the different cell lines[1]. ST1968 induces a comparable level of apoptosis in A431 and A431/TPT cells with IC50 of 0.21 and 0.29 μM[2].
Namitecan (10 mg/kg) in combination with cetuximab (1 mg/mouse) induces synergistic antitumor effects in SCC models as a function of EGFR gene copy number[1]. ST1968 (25 mg/kg) causes acceptable body weight loss and no toxic deaths. ST1968 produces a 100% complete response rate in the mice bearing the A431 tumor, and retains a relevant activity in the topotecan-resistant tumor[2].
[1]. De Cesare M, et al. Synergistic antitumor activity of cetuximab and namitecan in human squamous cell carcinoma models relies on cooperative inhibition of EGFR expression and depends on high EGFR gene copy number. Clin Cancer Res. 2014 Feb 15;20(4):995-1006. [2]. Zuco V, et al. Efficacy of ST1968 (namitecan) on a topotecan-resistant squamous cell carcinoma. Biochem Pharmacol. 2010 Feb 15;79(4):535-41.
Cell experiment: | The antiproliferative activity is evaluated after 72 hours of drug exposure by cell counting. Drug concentrations able to inhibit cell proliferation by 50% (IC50) and 20% (IC20) are calculated from dose-response curves. |
Animal experiment: | To generate tumor xenografts, exponentially growing cells (A431 and A431/topotecan, 107 cells/mouse; SiHa 2.5 × 107 cells/mouse, Caski 107 cells/mouse) are s.c. injected into the mice flanks. For antitumor activity studies, groups of four/five mice bearing tumor implanted in both flanks are used. Tumor fragments are implanted on day 0, and tumor growth is followed by biweekly measurements of tumor diameters with a Vernier caliper. Tumor volume (TV) is calculated according to the formula TV (mm3) = d2 × D/2, in which d and D are the shortest and the longest diameter, respectively. Treatment starts 5 to 13 days after implant, when the tumors are just palpable, but established (TV = 80-90 mm3). Namitecan, irinotecan, and cetuximab are administered every fourth day for four times. Cetuximab is given 1 hour after each administration of the camptothecin. |
References: [1]. De Cesare M, et al. Synergistic antitumor activity of cetuximab and namitecan in human squamous cell carcinoma models relies on cooperative inhibition of EGFR expression and depends on high EGFR gene copy number. Clin Cancer Res. 2014 Feb 15;20(4):995-1006. | |
| Cas No. | 372105-27-6 | SDF | |
| 别名 | ST-1968 | ||
| Canonical SMILES | O=C1[C@](O)(CC)C2=C(CO1)C(N3CC4=C(/C=N/OCCN)C5=CC=CC=C5N=C4C3=C2)=O | ||
| 分子式 | C23H22N4O5 | 分子量 | 434.44 |
| 溶解度 | DMSO: 250 mg/mL (575.45 mM) | 储存条件 | 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℃，然后在超声波浴中震荡一段时间。 |
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| 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。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3018 mL | 11.5091 mL | 23.0181 mL |
| 5 mM | 0.4604 mL | 2.3018 mL | 4.6036 mL |
| 10 mM | 0.2302 mL | 1.1509 mL | 2.3018 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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