LLS30

• CAS: 2138367-58-3
• Catalog Number: ACM2138367583
• Category: Inhibitors
• Molecular Weight: 701.47
• Molecular Formula: C34H33Cl4N5O3
• Description: LLS30 is an allosteric inhibitor of Galectin-1 (Gal-1). LLS30 decreases Gal-1 binding affinity to its binding partners, and potentially overcomes metastatic castration-resistant prostate cancer (mCRPC).
• Synonyms: LLS-30; LLS 30; LLS30
• IUPAC Name: 3-(2-(4-(Bis(2-hydroxyethyl)amino)phenyl)-1-(3,4-dichlorobenzyl)-1H-benzo[d]imidazol-5-yl)-3-((3,4-dichlorobenzyl)amino)propanamide
• Canonical SMILES: O=C(N)CC(C1=CC=C2N(CC3=CC=C(Cl)C(Cl)=C3)C(C4=CC=C(N(CCO)CCO)C=C4)=NC2=C1)NCC5=CC=C(Cl)C(Cl)=C5
• InChI: InChI=1S/C34H33Cl4N5O3/c35-26-8-1-21(15-28(26)37)19-40-30(18-33(39)46)24-5-10-32-31(17-24)41-34(43(32)20-22-2-9-27(36)29(38)16-22)23-3-6-25(7-4-23)42(11-13-44)12-14-45/h1-10,15-17,30,40,44-45H,11-14,18-20H2,(H2,39,46)
• InChI Key: XWBTXDFCKRACTA-UHFFFAOYSA-N
• Solubility: Soluble in DMSO
• Appearance: Solid powder
• Shelf Life: >3 years if stored properly
• Storage: Dry, dark and at 0-4 °C for short term (days to weeks) or -20 °C for long term (months to years).
• Biological Target: LLS30 is an allosteric inhibitor of Galectin-1 (Gal-1).
• Drug Formulation: This drug may be formulated in DMSO
• Elemental Analysis: C, 58.22; H, 4.74; Cl, 20.21; N, 9.98; O, 6.84
• Exact Mass: 699.1338
• HS Tariff Code: 2934.99.03.00
• In Vitro Activity: It was evaluated whether LLS30 could have an effect on the phosphorylation of Akt. Western blotting of cell lysates collected from CRPC PC3 (AR negative) and 22RV1 (AR positive) cells treated by LLS30 or DMSO showed that LLS30 treatment induced expression of p21, a cyclin-dependent kinase (CDK) inhibitor that interacts with Akt and also regulates survival. Phosphorylated AKT was partially suppressed in PC3 and 22RV1 cells after 24 hr treatment with 10 μM LLS30. Interestingly, treatment with LLS30 as well as siRNA knockdown of Gal-1, also decreased expression of AR and AR-Variants (AR-Vs) in 22RV1 cells. These results indicated that LLS30 inhibited CRPC cell growth through the suppression of Akt and AR pathway, and induction of p21. Moreover, these effects are most likely mediated through the inhibition of Gal-1 function.; Reference: Clin Cancer Res. 2018 Sep 1;24(17):4319-4331. https://pubmed.ncbi.nlm.nih.gov/29666302/
• In Vivo Activity: The invasion-inhibitory activity of LLS30 was measured in vivo. Luciferase-tagged PC3 cells were transplanted into nude mice via tail-vein injection, followed by LLS30 treatment (5mg/kg q.d.X5) two weeks later. In control groups, metastatic colonization was observed in all 6 mice in a period of six weeks after injection. PC3 cells are spread to major visceral organs, such as kidneys, lungs, livers, and spleens. In LLS30 treated group, only 1 mouse developed metastases. These results indicated that LLS30 is capable of inhibiting tumor invasion and metastasis in vivo.; Reference: Clin Cancer Res. 2018 Sep 1;24(17):4319-4331. https://pubmed.ncbi.nlm.nih.gov/29666302/
• Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
• Stock Solution Storage: 0-4 °C for short term (days to weeks), or -20 °C for long term (months).