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M5972735

Trabectedin , >95% , 114899-77-3

CAS NO.:114899-77-3

Empirical Formula: C39H43N3O11S

Molecular Weight: 761.84

MDL number: MFCD00874849

Pack Size Price Stock Quantity
1mg RMB19484.00 In Stock
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Update time: 2022-07-08

PRODUCT Properties

Melting point: >143°C (dec.)
alpha  D25 +114° (c = 0.1 in methanol)
Density  1.55±0.1 g/cm3 (20 ºC 760 Torr)
storage temp.  -20°C Freezer, Under inert atmosphere
solubility  Chloroform (Slightly), Methanol (Slightly)
pka 9.73±0.40(Predicted)
form  Solid
color  Light Yellow to Yellow
optical activity -53.824.5 (CHCl3)
InChIKey PKVRCIRHQMSYJX-HAHYLZASNA-N

Description and Uses

Trabectedin is a marine natural product derived from the tunicate Ecteinascidia turbinate. With its demonstrated in vitro and in vivo activity against a range of solid tumor cell lines, human xenografts and tumor explants, this antineoplastic agent has been developed and launched for the treatment of advanced STS after failure of first-line therapy with anthracyclines or ifosfamide or in patients who are unsuited to receive these agents. Its proposed mechanism of action involves binding to the N2 position of guanine in the minor groove demonstrating a preference for sequences containing 5′-PuGC and 5′-PyGG motifs. Subsequent alkylation of DNA, via an iminium intermediate generated from an intra-molecular acid-catalyzed activation and dehydration of the carbinolamine, induces a curvature of the DNA toward the major groove that ultimately disrupts the binding of transcription factors involved in cell proliferation. Evaluation of trabectedin against the National Cancer Institute’s human in vitro cell line panel, including melanoma, non-small-cell lung, ovarian, renal, prostate, and breast cancer, demonstrated potencies ranging from 1 pM to 10 nM.

A tetrahydroisoquinoline alkaloid with antitumor activity isolated from the Caribbean tunicate, Ecteinascidin turbinata. It is the first marine anticancer agent approved in the European Union for patients with soft tissue sarcoma (STS). Antineoplastic.

Safety

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