Ecteinascidin 770


Catalog No. Size PriceQuantity
M12688-2 2mg solid $245
M12688-10 10mg solid $930

Description

Ecteinascidin 770 (ET-770) is a 1, 2, 3, 4-tetrahydroisoquinoline alkaloid with potent anti-cancer activities; inhibits U373MG cells with an IC50 of 4.83 nM.

Product information

CAS Number: 114899-80-8

Molecular Weight: 770.85

Formula: C40H42N4O10S

Synonym:

Ecteinascidine 770

Et-770

Chemical Name: [(1R, 2R, 3R, 11S, 12R, 14R, 26R)-12-cyano-5, 6'-dihydroxy-6, 7'-dimethoxy-7, 21, 30-trimethyl-27-oxospiro[17, 19, 28-trioxa-24-thia-13, 30-diazaheptacyclo[12.9.6.13, 11.02, 13.04, 9.015, 23.016, 20]triaconta-4(9), 5, 7, 15, 20, 22-hexaene-26, 1'-3, 4-dihydro-2H-isoquinoline]-22-yl] acetate

Smiles: CN1[C@H]2[C@@H]3[C@@H]4SC[C@]5(NCCC6=CC(O)=C(C=C56)OC)C(=O)OC[C@@H](C5C4=C(OC(C)=O)C(C)=C4OCOC4=5)N3[C@@H](C#N)[C@@H]1CC1=CC(C)=C(OC)C(O)=C12

InChiKey: BGFXHQYUWCGGLL-QWIBJBKUSA-N

InChi: InChI=1S/C40H42N4O10S/c1-17-9-21-10-23-24(13-41)44-25-14-51-39(48)40(22-12-27(49-5)26(46)11-20(22)7-8-42-40)15-55-38(32(44)31(43(23)4)28(21)33(47)34(17)50-6)30-29(25)37-36(52-16-53-37)18(2)35(30)54-19(3)45/h9,11-12,23-25,31-32,38,42,46-47H,7-8,10,14-16H2,1-6H3/t23-,24-,25-,31+,32+,38+,40+/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Ecteinascidin 770 induces apoptosis of U373MG cells. The IC50 concentration of ecteinascidin 770 for killing U373MG glioblastoma cells in culture by using the MTT assay is 4.83 nM by a 72 hour-treatment. The IC50 values against human cell lines HCT116, QG56, and DU145 are 0.6, 2.4, and 0.81 nM, respectively. ET-770 is shown to enhance anoikis response of human lung cancer H23 cells in a dose-dependent manner. Ecteinascidin 770 sensitizes the cells by activating the p53 protein, which in turn down-regulates anti-apoptotic myeloid cell leukemia sequence-1 (MCL1) and up-regulates BCL2-associated X protein (BAX) proteins. However, B-cell lymphoma-2 (BCL2) proteins are not significantly affected by Ecteinascidin 770. The anoikis sensitization of ET-770 is observed in H460 lung cancer cells.

References:

  1. Tabunoki H, et al. Molecular network profiling of U373MG human glioblastoma cells following induction of apoptosis by novel marine-derived anti-cancer 1,2,3,4-tetrahydroisoquinoline alkaloids. Cancer Cell Int. 2012 Apr 11;12(1):14.
  2. Saktrakulkla P, et al. Chemistry of ecteinascidins. Part 3: preparation of 2'-N-acyl derivatives of ecteinascidin 770 and evaluation of cytotoxicity. Bioorg Med Chem. 2011 Aug 1;19(15):4421-36.
  3. Powan P, et al. Ecteinascidin 770, a tetrahydroisoquinoline alkaloid, sensitizes human lung cancer cells to anoikis. Anticancer Res. 2013 Feb;33(2):505-12.

Products are for research use only. Not for human use.

Payment & Security

American Express Diners Club Discover JCB Mastercard PayPal Venmo Visa

Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.

Estimate shipping

You may also like

Recently viewed