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Ansicin p-3 is a chemical precursor of the antitumor drug DM1. DM1 is a small chemical molecule synthesized by chemical modification of a chemotherapeutic drug called medenol. DM1 can be prepared into a targeted anti-tumor drug by coupling the linker molecule with a targeted antibody, reducing the side effects of chemotherapy and enhancing the efficacy. Roche's new drug T-DM1(trastuzumab DM1, Trastuzumab DM1) for the treatment of breast cancer, which is a conjugate drug of the antibody drug Herceptin-DM1, was used in advanced breast cancer patients to delay the development of tumor growth by 3.2 months compared to lapatinib.
Uses and functions of ansamitocin P-3.
Ansamitocin P-3(AP3) is a small fraction of Ansa antibiotics, which has many pharmacological activities such as anti-tumor, anti-tuberculosis bacillus and anti-bacteria. Its components are P-0, P-1, P-2, P-3, P-3', P-4 and P-4', among which ansicin P-3 is the main synthetic product, which prevents cell death by preventing microtubule formation, and has significant anti-tumor effects in vitro and in tumor-bearing animals.
Preparation method of ansamitocin P-3.
1) The fermentation liquid or solid fermentation medium at the end of the fermentation is extracted with extraction solvent to obtain the extraction liquid;
2) Concentrate the extraction liquid obtained in step 1 until no extraction solvent flows out to get concentrated extract crude A, then add neutral alumina, and mix it evenly with crude A with organic solvent;
3) Steam the evenly mixed coarse product A of step 2 until it is dry and sandy;
4) Add the organic solvent to the dry sandy coarse product A in step 3, leave it in shock and take the supernatant;
5) Concentrate the supernatant of step 4, add silica gel and spin steam to sand, then gradient elution by column chromatography to obtain ansicin P-3.
Product method of Bulk ansamitocin P-3.
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