Tubulin inhibitor 1
目录号 : GC33291
Tubulininhibitor1是tubulin抑制剂，靶作用于秋水仙素结合位点，抑制微管蛋白聚集。Tubulininhibitor1具有抗肿瘤活性，能够导致细胞G2/M期有丝分裂停滞，诱导细胞凋亡。
Cas No.:2237054-53-2
Sample solution is provided at 25 µL, 10mM.
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Tubulin inhibitor 1 is a tubulin inhibitor, occupying the colchicine binding site, inhibits tubulin polymerization. Tubulin inhibitor 1 shows potent anti-tumor activity, casues cellular mitotic arrest in the G2/M phase, and induces cellular apoptosis[1].
Tubulin inhibitor 1 (Compound 7a3) is a tubulin inhibitor, occupying the colchicine binding site, inhibits tubulin polymerization[1].Tubulin inhibitor 1 has potent anti-proliferative activity against SK-OV-3, MDA-MB-231, HeLa, A549, CT26 and MCF-7 cells, with IC50s of 16.7 ± 3.0, 31.4 ± 0.7, 32.8 ± 2.9, 67.0 ± 0.8, 58.0 ± 2.4 and 35.4 ± 5.6 nM, respectively[1].Tubulin inhibitor 1 (40, 80, and 160 nM, 48 hours) markedly causes cellular mitotic arrest in the G2/M phase, induces apoptosis in SK-OV-3 cells[1].|| Apoptosis Analysis[1]||Cell Line:|SK-OV-3 cells|Concentration:|40, 80, and 160 nM|Incubation Time:|48 h|Result:|Induced apoptosis in SK-OV-3 cells after treatment for 48 h.
Tubulin inhibitor 1 (50 mg/kg, i.p., every two days three times for 20-25 days) is well tolerated, significantly reduces tumour growth in Balb/c nude mice bearing SK-OV-3 cells[1].|| Animal Model:|Six-week-old Balb/c nude mice (18-20 g) beraring SK-OV-3 cells[1]|Dosage:|50 mg/kg|Administration:|I.P., every two days three times for 20-25 days|Result:|Significantly reduced tumour growth in Balb/c nude mice bearing SK-OV-3 cells, without obvious body weight loss.
[1]. Lai Q, et al. Design, synthesis and biological evaluation of a novel tubulin inhibitor 7a3 targeting the colchicine binding site. Eur J Med Chem. 2018 Aug 5;156:162-179.
| Cas No. | 2237054-53-2 | SDF | |
| Canonical SMILES | CCOC1=CC=C(C2=CN(C)N=C2C3=CC(OC)=C(OC)C(OC)=C3)C=C1 | ||
| 分子式 | C21H24N2O4 | 分子量 | 368.43 |
| 溶解度 | DMSO : ≥ 125 mg/mL (339.28 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 | 2.7142 mL | 13.5711 mL | 27.1422 mL |
| 5 mM | 0.5428 mL | 2.7142 mL | 5.4284 mL |
| 10 mM | 0.2714 mL | 1.3571 mL | 2.7142 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
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet