Toyocamycin
(Synonyms: 丰加霉素; Vengicide) 目录号 : GC11805
A natural antibiotic and IRE1α inhibitor
Cas No.:606-58-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
three MM cell lines, RPMI8226, XG7 and U266 |
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Preparation method |
The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
0.01, 0.03 and 0.1 μM; 24 h |
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Applications |
In RPMI8226 cells, treatment with 10 nM or higher concentrations of toyocamycin reduced the levels of spliced isoform of XBP1 protein and resulted in caspase activation. Toyocamycin also reduced the levels of spliced-XBP1 in two other MM cell lines XG7 and U266. Toyocamycin also inhibited thapsigargin-induced expression of spliced XBP1 protein. |
| Animal experiment [1]: | |
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Animal models |
SCID mice bearing human MM RPMI8226 xenograft |
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Dosage form |
intraperitoneal injection, 0.5mg/kg twice weekly or 1.0mg/kg once weekly for 2 weeks. |
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Application |
In SCID mice bearing human MM RPMI8226 xenograft, Toyocamycin alone showed robust anti-tumor activity resulting in smaller tumor volumes compared with controls on day 15. The combination treatment of BTZ with toyocamycin showed a trend toward enhancing anti-tumor activity. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Ri M, Tashiro E, Oikawa D, et al, Identification of Toyocamycin,an agent cytotoxic for multiple myeloma cells, as a potent inhibitor of ER stress-induced XBP1 mRNA splicing. Blood Cancer J. 2012 Jul;2(7):e79. |
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Toyocamycin is an inhibitor of phosphatidylinositol kinase. It is known as an antifungal antibiotic. [1]
Phosphatidylinositol kinase is one of the important enzymes that take part in the regulation of the pathway of phosphatidylinositol turnover. Phosphatidylinositol turnover is studied to be involved in the cellular response to mitogens and transformation.[1]
Toyocamycin can suppress thapsigargin-, tunicamycin- and 2-deoxyglucose-induced XBP1 mRNA splicing in HeLa cells. This suppression doesn’t affect the activating of transcription factor 6 (ATF6) and PKR-like ER kinase (PERK)’s activation. Toyocamycin prevents IRE1a-induced XBP1 mRNA cleavage in vitro. [2]
In mammalian cells, toyocamycin inhibits RNA synthesis. Toyocamycin induces apoptosis of MM cells including bortezomib-resistant cells at nanomolar levels in a dose-dependent manner. It also inhibited growth of xenografts in an in vivo model of human multiple myeloma. It is also a lead compound for developing anti-MM therapy and XBP1 as an appropriate molecular target for anti-multiple myeloma therapy.[2]
References:
[1]Nishioka H, Sawa T, etal. , Inhibition of phosphatidylinositol kinase by toyocamycin. J Antibiot (Tokyo). 1990 Dec;43(12):1586-9.
[2]Ri M, Tashiro E, Oikawa D, etal. , Identification of Toyocamycin,an agent cytotoxic for multiple myeloma cells, as a potent inhibitor of ER stress-induced XBP1 mRNA splicing. Blood Cancer J. 2012 Jul;2(7):e79.
| Cas No. | 606-58-6 | SDF | |
| 别名 | 丰加霉素; Vengicide | ||
| 化学名 | 4-amino-7-((2S,3R,4R,5S)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile | ||
| Canonical SMILES | O[C@H]1[C@@H](N2C3=NC=NC(N)=C3C(C#N)=C2)O[C@@H](CO)[C@@H]1O | ||
| 分子式 | C12H13N5O4 | 分子量 | 291.26 |
| 溶解度 | Soluble in DMSO | 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.4334 mL | 17.1668 mL | 34.3336 mL |
| 5 mM | 0.6867 mL | 3.4334 mL | 6.8667 mL |
| 10 mM | 0.3433 mL | 1.7167 mL | 3.4334 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。