| CAS NO: | 129298-91-5 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 401.9 |
| Cas No. | 129298-91-5 |
| Formula | C19H28ClNO6 |
| Synonyms | AGM-1470|O-(Chloroacetyl-carbamoyl) Fumagillol|NSC 642492 |
| Solubility | ≤10mg/ml in ethanol;10mg/ml in DMSO;10mg/ml in dimethyl formamide |
| Chemical Name | (3R,4S,5S,6R)-5-methoxy-4-[(2R,3R)-2-methyl-3-(3-methyl-2-buten-1-yl)-2-oxiranyl]-1-oxaspiro[2.5]oct-6-yl ester N-(2-chloroacetyl)-carbamic acid |
| Canonical SMILES | O=C(NC(CCl)=O)O[C@@H]1CC[C@@]2(OC2)[C@]([C@](O3)(C)[C@H]3C/C=C(C)/C)([H])[C@@H]1OC |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
IC50: 2 μM
TNP-470 is a methionine aminopeptidase-2 (MetAP2) inhibitor.
MetAP2 is present in all organisms and is important due to its key role in tissue repair and protein degradation. Moreover, MetAP2 is of particular interest since it plays a critical role in angiogenesis, which is necessary for the progression of diseases, such as solid tumor cancers and rheumatoid arthritis.
In vitro: Antitumor activity of TNP-470 was evaluated in eight human cultured cell lines derived from choriocarcinoma; ovarian cancer; TYK and Nakajima; and uterine endometrial cancer. Results showed that after 7-day culture with TNP-470, in medium at the concentration of 10 to 10-2 μg/ml, the inhibition of growth was observed in all of the eight cell lines. The half inhibitory concentration of choriocarcinoma cell lines was at an extremely low level compared to that of e uterine endometrial cancer and pithelial ovarian cancer [1].
In vivo: The anti-tumor effect of TNP-470 was studied using nude mice with tumors of GCH-1(m), NUC-1, or Nakajima cells. When the size of the transplanted tumor reached 100–200 mm3, 3, 10, or 30 mg/kg of TNP-470 was injected every other day. It was found that the inhibitory effect of TNP-470 was obtained by the administration of 10 and 30 mg/kg in GCH-1(m) and NUC-1 cells, respectively, while in Nakajima cells there was no significant effect. In addition, in nude mice treated with 30 mg/kg of TNP-470, lung metastasis of GCH-1(m) cells was greatly inhibited both in the number and the size of tumor nodules, suggesting that the capillary growth in the originally developed tumor was also reduced [1].
Clinical trial: A phase I study found that the effects of TNP-470 could be evaluated in 32 of the 33 patients. The dose-limiting toxic effect was a characteristic neuropsychiatric symptom complex. No definite anti-tumor activity of TNP-470 was observed; however, transient stimulation of the serum prostate-specific antigen concentration occurred in some of the patients treated [2].
References:
[1] T. Yanase, M. Tamura, K. Rujita, et al. Inhibitory effect of angiogenesis inhibitor TNP-470 on tumor growth and metastasis of human cell lines in vitro and in vivo. Cancer Research 53(11), 2566-2570 (1993).
[2] C J Logothetis et al. Phase I trial of the angiogenesis inhibitor TNP-470 for progressive androgen-independent prostate cancer. Clinical Cancer Research 7(5):1198-203.
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