SB 218078
目录号 : GC11022
A potent Chk1 inhibitor
Cas No.:135897-06-2
Sample solution is provided at 25 µL, 10mM.
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Targets:Chk1, cdc2 and PKC
IC50:15, 250 and 1000 nM for Chk1, cdc2 and PKC respectively
SB 218078 is a potent inhibitor of checkpoint kinase 1, with the IC50 values of 15, 250 and 1000 nM for Chk1, cdc2 and PKC, respectively.
In Vitro: An in vitro kinase assay found that SB 218078 could potently inhibit the phosphorylation of Chk1, with the IC50 of 15 nM. In Hela cells, SB 218078 could cause complete abrogation of G2 cell cycle arrest induced by topotecan, with the minimum concentration of 2.5 μM [1]. Besides, 15 nM SB 218078 could effectively inhibit NKG2D ligand upregulation induced by aphidicolin in fibroblasts [2]. Furthermore, treated GM02188 cells with 2.5 μM SB 218078 could inhibit the formation of HU-induced 53bp1 foci and prevent recovery from replication fork stalling induced by APH [3].
In Vivo: In Myc-induced lymphomas mouse model, treatment with SB 218078 with the dose of 5 mg/kg could promote a strong increase of γ-H2AX and apoptosis throughout the lymphoma, while having no effect on a healthy spleen [4].
Clinical trial: No data available recently
References:
[1] Jackson J R, Gilmartin A G, Imburgia C S, et al. An Indolocarbazole Inhibitor of Human Checkpoint Kinase (Chk1) Abrogates Cell Cycle Arrest Caused by DNA Damage[J]. Cancer Research, 2000, 60(3): 566-572.
[2] Gasser S, Orsulic S, Brown E J, et al. The DNA damage pathway regulates innate immune system ligands of the NKG2D receptor[J]. Nature, 2005, 436(7054): 1186-1190.
[3] Alderton G K, Galbiati L, Griffith E, et al. Regulation of mitotic entry by microcephalin and its overlap with ATR signalling[J]. Nature Cell Biology, 2006, 8(7): 725-733.
[4] Murga M, Campaner S, Lopez-Contreras A J, et al. Exploiting oncogene-induced replicative stress for the selective killing of Myc-driven tumors[J]. Nature structural & molecular biology, 2011, 18(12): 1331-1335.
| Cas No. | 135897-06-2 | SDF | |
| 化学名 | 9,10,11,12-tetrahydro-9,12-epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-1,3(2H)-dione | ||
| Canonical SMILES | O=C(NC1=O)C2=C1C3=C4C5=C2C6=C(C=CC=C6)N5C7OC(CC7)N4C8=C3C=CC=C8 | ||
| 分子式 | C24H15N3O3 | 分子量 | 393.4 |
| 溶解度 | ≤5mg/ml in DMSO;5mg/ml in dimethyl formamide | 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 | 2.5419 mL | 12.7097 mL | 25.4194 mL |
| 5 mM | 0.5084 mL | 2.5419 mL | 5.0839 mL |
| 10 mM | 0.2542 mL | 1.271 mL | 2.5419 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet