| Chemical Properties | Back Directory | [density ]
1.39±0.1 g/cm3(Predicted) | [storage temp. ]
-10 to -25°C | [solubility ]
DMSO:20.0(Max Conc. mg/mL);12.97(Max Conc. mM)
Ethanol:10.0(Max Conc. mg/mL);6.48(Max Conc. mM) | [form ]
Solid | [pka]
4.60±0.10(Predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Biological Activity]
DT2216 is a selective BCL-XLbut not BCL-2 or BCL-Wdegrader composed of a von Hippel-Lindau (VHL) E3 ligase-targeting ligand linked to a ABT-263 (navitoclax) derivative. DT2216 is more potent than ABT-263 against BCL-XL-dependent leukemia (MOLT-4 IC50 = 52 vs 191 nM) and cancer cells (MDA-MB-231 IC50 = 229 vs 707 nM). DT2216 effectively inhibits the growth of several xenograft tumors in vivo either alone (15 mg/kg/wk i.p.) or in combination with other chemotherapeutic agents (docetaxel or VDL)exhbiting improved efficacy and reduced thrombocytopenia when compared with ABT-263 as a result of greatly reduced platelet toxicity due to poor VHL expression in platelets. |
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