1632032-53-1

Basic information

• Product Name: LB-100
• Synonyms: endothall 4-methylpiperazine monoamide
• CAS NO: 1632032-53-1
• Molecular Formula: C13H20N2O4
• Molecular Weight: 268.3089
• Mol File: 1632032-53-1.mol

Chemical Properties

• Boiling Point: 486.9±45.0 °C(Predicted)
• Appearance: /
• Density: 1.312±0.06 g/cm3(Predicted)
• PKA: 4.03±0.40(Predicted)
• CAS DataBase Reference: LB-100(CAS DataBase Reference)
• NIST Chemistry Reference: LB-100(1632032-53-1)
• EPA Substance Registry System: LB-100(1632032-53-1)

Safety Data

• Hazardous Substances Data: 1632032-53-1(Hazardous Substances Data)

Upstream product

• 109-01-3 1-methyl-piperazine 
• 29745-04-8 norcantharidin 
• 1164475-59-5 7-oxabicyclo[2,2,1]heptane-2,3-dicarboxylic acid anhydride 

Relevant articles and documents

Heterocyclic substituted cantharidin and norcantharidin analogues-synthesis, protein phosphatase (1 and 2A) inhibition, and anti-cancer activity

Norcantharidin (3) is a potent PP1 (IC50 = 9.0 ± 1.4 μM) and PP2A (IC50 = 3.0 ± 0.4 μM) inhibitor with 3-fold PP2A selectivity and induces growth inhibition (GI50 ～45 μM) across a range of human cancer cell lines including those of colorectal (HT29, SW480), breast (MCF-7), ovarian (A2780), lung (H460), skin (A431), prostate (DU145), neuroblastoma (BE2-C), and glioblastoma (SJ-G2) origin. Until now limited modifications to the parent compound have been tolerated. Surprisingly, simple heterocyclic half-acid norcantharidin analogues are more active than the original lead compound, with the morphilino-substituted (9) being a more potent (IC50 = 2.8 ± 0.10 μM) and selective (4.6-fold) PP2A inhibitor with greater in vitro cytotoxicity (GI50 ～9.6 μM) relative to norcantharidin. The analogous thiomorpholine-substituted (10) displays increased PP1 inhibition (IC50 = 3.2 ± 0 μM) and reduced PP2A inhibition (IC50 = 5.1 ± 0.41 μM), to norcantharidin. Synthesis of the analogous cantharidin analogue (19) with incorporation of the amine nitrogen into the heterocycle further increases PP1 (IC50 = 5.9 ± 2.2 μM) and PP2A (IC50 = 0.79 ± 0.1 μM) inhibition and cell cytotoxicity (GI50 ～3.3 μM). These analogues represent the most potent cantharidin analogues thus reported. Crown Copyright

PROCESS OF SYNTHESIZING 3-(4-METHYLPIPERAZINE-1-CARBONYL)-7-OXABICYCLO[2.2.1] HEPTANE-2-CARBOXYLIC ACID

The present invention provides a process for producing the compound having the structure: (formula) comprising, (a) reacting a compound having the structure : (formula) with a compound having the structure: (formula) in the presence of a first organic sol

Oxabicycloheptanes and oxabicylcoheptenes, their preparation and use

This invention provides compounds having the structure which may be used for the treatment of tumors.