Maitansin Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

This novel ansa macrolide alkaloid occurs in a number of May tan us species. The structure given has been elucidated from chemical and spectroscopic data. In low doses (25-50 mcg/kg), maytansine prolonged the survival of mice bearing vincristine-sensitive P388 leukemia but not those bearing vincristine-resistant tumour lines. In vitro, it suppressed the growth of U21 0, LSl78Y and P388 leukemia cells with ED₅₀ of 2 X 10^-9 , 1.5 X 10^-9 and 6 X 10^-10M respectively and elevated the mitotic index in L 121 0 cells. From labelling studies it was shown that the alkaloid inhibited DNA formation by P388 cells to a greater extent than RNA and protein synthesis. Maytensine did not inhibit RNA polymerase from Escherichia coli at levels as high as 1 X 10^-4M.

Verwenden

Antineoplastic.

Definition

ChEBI: An organic heterotetracyclic compound and 19-membered macrocyclic lactam antibiotic originally isolated from the Ethiopian shrub Maytenus serrata but also found in other Maytenus species. It exhibits cytotoxicity against many tumo r cell lines.

Biologische Funktion

Maytansine is a potent microtubule-targeted compound that inhibits proliferation of cells at mitosis. Antibody-maytansinoid conjugates consisting of maytansinoids (DM1 and DM4) attached to tumor-specific antibodies have shown promising clinical results The microtubule-targeting maytansinoids accumulate in cells and induce mitotic arrest at 250- to 1000-fold lower concentrations than those required for their association with tubulin or microtubules.

Toxikologie

Maytansine, an ansa macrolide isolated from African plants of the genera Maytenus and Putterlickia was first described almost two decades ago. It had been reported to be active against several forms of cancer, but a later phase II evaluation suggested no major role for this drug in tumor treatment. Although the toxic side effects were moderate, the antitumor activity was also not impressive.
Maytansine binds to tubulin rapidly and reversibly. Competitive inhibition of binding between maytansine and the vinca alkaloids has been observed, suggesting that maytansine must occupy at least one of vinblastine's binding sites on the tubulin molecule. The number of the maytansine binding sites is not known. Assembly of MT is inhibited at maytansine concentrations below 1μM. This suggests a substoichiometric poisoning mechanism as in the cases of colchicine, vinblastine and podophyllotoxin, but the details are not known. In contrast to many other MT-interacting toxins，maytansine does not promote the formation of aberrant tubulin polymers, even at millimolar concentrations. In fact, low concentrations of maytansine even inhibit vinblastine-induced formation of aberrant polymers.

Einzelnachweise

Walpert-Defillipes et al., Biochem. Pharmacol., 24, 751 (1975)

Maitansin Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte

Maitansin Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

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BOC Sciences	16314854226; +16314854226	inquiry@bocsci.com	United States	19741	58
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	32957	60
TargetMol Chemicals Inc.	+1-781-999-5354 +1-00000000000	marketing@targetmol.com	United States	32161	58
Hubei Ipure Biology Co., Ltd	+8613367258412	ada@ipurechemical.com	China	10319	58
Career Henan Chemica Co	+86-0371-86658258 +8613203830695	laboratory@coreychem.com	China	30239	58
Wuhan Monad Medicine Tech Co.,LTD	02768782018 18771942761	sales01@whmonad.com	CHINA	979	58
ANHUI WITOP BIOTECH CO., LTD	+8615255079626	eric@witopchemical.com	China	23541	58
Dorne Chemical Technology co. LTD	+86-86-13583358881 +8618560316533	Ethan@dornechem.com	China	3096	58
Alfa Chemistry		Info@alfa-chemistry.com	United States	24072	58
InvivoChem	+1-708-310-1919 +1-13798911105	sales@invivochem.cn	United States	6391	58

35846-53-8(Maitansin)Verwandte Suche:

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