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DT2216 inhibits various Bcl-XL-dependent leukemias and cancer cells, but is significantly less toxic to platelets.DT2216 is a selective B-cell lymphoma, extremely large (BCL-XL), proteolytic targeting chimera (PROTAC).DT2216 targets bcl-XL to the Von Hippel-Lindau (VHL) E3 ligase for degradation.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $71 | In Stock | |
5 mg | $289 | In Stock | |
10 mg | $463 | In Stock | |
25 mg | $928 | In Stock | |
50 mg | $1,480 | In Stock | |
100 mg | $2,380 | In Stock |
Description | DT2216 inhibits various Bcl-XL-dependent leukemias and cancer cells, but is significantly less toxic to platelets.DT2216 is a selective B-cell lymphoma, extremely large (BCL-XL), proteolytic targeting chimera (PROTAC).DT2216 targets bcl-XL to the Von Hipp |
In vitro | DT2216 (0.1, 0.3 μM; 24 hours) kills MOLT-4 cells by caspase-3-mediated induction of apoptosis in a BCL-2 homologous antagonist killer (BAK)- and BCL-2-associated X protein (BAX)-dependent manner.DT2216 (62.5, 125 nM; 72?hours) kills MOLT-4 cells. DT2216 (0.001-10 μM; 72?hour) shows highly toxic to MOLT-4 cells with an EC50 of 0.052 μM. |
In vivo | DT2216 (i.p.; 7.5, 15 mg/kg; weekly for 60 days) of 15 mg/kg is more effective at suppressing the growth of MOLT-4 T-ALL xenografts in mice than 7.5 mg/kg. |
Molecular Weight | 1542.36 |
Formula | C77H96ClF3N10O10S4 |
Cas No. | 2365172-42-3 |
Smiles | CC1(C)CCC(C2=CC=C(Cl)C=C2)=C(C1)CN3CCN(C4=CC=C(C(NS(=O)(C5=CC(S(C(F)(F)F)(=O)=O)=C(N[C@@H](CSC6=CC=CC=C6)CCN7CCN(C(CCCCCC(N[C@@H](C(C)(C)C)C(N8[C@@H](C[C@@H](O)C8)C(N[C@H](C9=CC=C(C%10=C(N=CS%10)C)C=C9)C)=O)=O)=O)=O)CC7)C=C5)=O)=O)C=C4)CC3 |
Relative Density. | 1.39 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
Solubility Information | DMSO: 25 mg/mL (16.21 mM), Sonication is recommended. H2O: < 0.1 mg/mL (insoluble) | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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