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TNP-470

Catalog No.
C3622
methionine aminopeptidase-2 (MetAP2) inhibitor
Grouped product items
SizePriceStock Qty
5mg
$104.00
Ship with 5-10 days
10mg
$198.00
Ship with 5-10 days
25mg
$469.00
Ship with 5-10 days

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

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.

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt401.9
Cas No.129298-91-5
FormulaC19H28ClNO6
SynonymsAGM-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
SDFDownload SDF
Canonical SMILESO=C(NC(CCl)=O)O[[email protected]@H]1CC[[email protected]@]2(OC2)[[email protected]]([[email protected]](O3)(C)[[email protected]]3C/C=C(C)/C)([H])[[email protected]@H]1OC
Shipping ConditionShip with blue ice, or upon other requests.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon.

Quality Control

Quality Control & MSDS

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Chemical structure

TNP-470