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Details

Stereochemistry ABSOLUTE
Molecular Formula C18H27N3O6
Molecular Weight 381.4235
Optical Activity UNSPECIFIED
Defined Stereocenters 3 / 3
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of TYROSERLEUTIDE

SMILES

CC(C)C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC1=CC=C(O)C=C1)C(O)=O

InChI

InChIKey=MQGGXGKQSVEQHR-KKUMJFAQSA-N
InChI=1S/C18H27N3O6/c1-10(2)7-14(18(26)27)20-17(25)15(9-22)21-16(24)13(19)8-11-3-5-12(23)6-4-11/h3-6,10,13-15,22-23H,7-9,19H2,1-2H3,(H,20,25)(H,21,24)(H,26,27)/t13-,14-,15-/m0/s1

HIDE SMILES / InChI

Description

Tyroserleutide (YSL) is a tripeptide treatment being developed by Shenzhen Kangzhe Pharmaceutical Co Ltd, a subsidary of China Medical System Holdings (CMS), for the treatment of liver cancer. It is initially separated and purified from the hydrolyzates of pig’s spleen, but now can be obtained by chemical synthesis, its chemical name is L-tyrosine-L-serine-L-leucine. Tyroserleutide is an active, low-molecular-weight polypeptide, comprised of three amino acids, that has shown antitumor effects on human hepatocarcinoma BEL-7402 in vitro and in vivo. Tyroserleutide has various advantages over the other bioactive peptides such as its low molecular weight, simple construction, nonimmunogenicity, specificity, few side effects, and ease of synthesis. Tyroserleutide is in Phase-III clinical trials for the treatment of liver cancer.

Originator

Approval Year

PubMed

Sample Use Guides

In Vivo Use Guide
Hepatocellular carcinoma: continuous administration of Tyroserleutide (YSL) by a portable infusion pump; forty patients (12 in stage 1, 28 in stage 2, total 10 treated in each dose cohort) were treated with Tyroserleutide 6, 12, 18, or 24 mg/day lasting for 5 days.
Route of Administration: Intravenous
In Vitro Use Guide
When B16-F10 cells were treated with Tyroserleutide (0.01, 0.1, 1, 10, or 100 ug/mL) in vitro, it inhibited the proliferation of B16-F10 cells with a 28.11% rate of inhibition.