solid , 120166-69-0

Synonym(s):
3-[2-[4-(bis(4-Fluorophenyl)methylene)-1-piperidinyl]ethyl]-2,3-dihydro-2-thioxo-4(1H)-quinazolinone;Diacylglycerol Kinase Inhibitor II - CAS 120166-69-0 - Calbiochem;R59949;R59949, 3-{2-[4-[ bis-(4-Fluorophenyl)methylene]-1-piperidinyl]ethyl}-2,3-dihydro-2-thioxo-4(1H)quinazolinone, DGK Inhibitor II;R59949, 3-{2-[4-[bis-(4-Fluorophenyl)methylene]-1-piperidinyl]ethyl}-2,3-dihydro-2-thioxo-4(1H)quinazolinone, DGK Inhibitor II

CAS NO.：120166-69-0

Empirical Formula: C28H25F2N3OS

Molecular Weight: 489.58

MDL number: MFCD00069258

PRODUCT Properties

• Melting point: 228-230 °C
• Boiling point: 637.1±65.0 °C(Predicted)
• Density: 1.36±0.1 g/cm3(Predicted)
• storage temp.: -20°C
• solubility: 0.1 M HCl: slightly soluble
• form: solid
• pka: 11.24±0.20(Predicted)
• color: pale yellow
• biological source: synthetic (organic)

Description and Uses

R-59-949 is an inhibitor of diacylglycerol kinase α (DGK-α) with an IC₅₀ value of 300 nM in isolated platelet plasma membranes using exogenous diacylglycerol as a substrate. DGK-α inhibition with R-59-949 increases diacylglycerol-dependent PKC activity, serotonin secretion, and aggregation of thrombin-stimulated platelets. R-59-949 inhibits DGK-α activity induced by platelet-derived growth factor (PDGF) in intact vascular smooth muscle cells (VSMCs). It inhibits high K⁺- and glucose-induced insulin secretion in MIN6 pancreatic β-cells in a dose-dependent manner. In vivo, administration of R-59-949 prevents retinal neovascularization in a mouse model of oxygen-induced retinopathy.

Diacylglycerol Kinase Inhibitor II has been used to determine tumor-induced inhibition with genetically modified cytotoxic T cells expressing chimeric antigen receptors (CAR). It has also been used to induce pAkt and PKR-like extracellular signal-regulated kinase (pErk) signals in T-cell acute lymphoblastic leukemia (T-ALL) cells.

Safety

• Symbol(GHS): GHS07
• Signal word: Warning
• Hazard statements: H335-H315-H319
• Precautionary statements: P264-P280-P302+P352-P321-P332+P313-P362-P264-P280-P305+P351+P338-P337+P313P
• Hazard Codes: Xi
• Risk Statements: 36/37/38
• Safety Statements: 26-36
• WGK Germany: 3