Description
DT2216-isomer is an isomer of DT2216. Compared to DT-2216, DT2216-isomer has a S-chiral carbon which links to the nitrogen atom of the aniline group. DT2216 is a potent and selective Bcl-xL-specific degrader. DT2216 is highly active against Bcl-xL-dependent T cell lymphomas. DT2216 selectively killed various Bcl-xL-dependent TCL cells including MyLa cells in vitro. In vivo, DT2216 alone was highly effective against MyLa TCL xenografts in mice without causing significant thrombocytopenia or other toxicity. Furthermore, DT2216 combined with ABT199 (a selective Bcl-2 inhibitor) synergistically reduced disease burden and improved survival in a TCL PDX mouse model dependent on both Bcl-2 and Bcl-xL.
Product information
Molecular Weight: 1542.36
Formula: C77H96ClF3N10O10S4
Smiles: CC(C)(C)[C@H](NC(=O)CCCCCC(=O)N1CCN(CC[C@@H](CSC2C=CC=CC=2)NC2=CC=C(C=C2S(=O)(=O)C(F)(F)F)S(=O)(=O)NC(=O)C2C=CC(=CC=2)N2CCN(CC2)CC2CC(C)(C)CCC=2C2C=CC(Cl)=CC=2)CC1)C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](C)C1C=CC(=CC=1)C1SC=NC=1C
InChiKey: PXVFFBGSTYQHRO-YDYQAAPMSA-N
InChi: InChI=1S/C77H96ClF3N10O10S4/c1-51(53-18-20-55(21-19-53)70-52(2)82-50-103-70)83-73(96)66-44-61(92)48-91(66)74(97)71(75(3,4)5)85-68(93)16-12-9-13-17-69(94)90-42-36-87(37-43-90)35-33-59(49-102-62-14-10-8-11-15-62)84-65-31-30-63(45-67(65)104(98,99)77(79,80)81)105(100,101)86-72(95)56-24-28-60(29-25-56)89-40-38-88(39-41-89)47-57-46-76(6,7)34-32-64(57)54-22-26-58(78)27-23-54/h8,10-11,14-15,18-31,45,50-51,59,61,66,71,84,92H,9,12-13,16-17,32-44,46-49H2,1-7H3,(H,83,96)(H,85,93)(H,86,95)/t51-,59-,61+,66-,71+/m0/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: To be determined
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
References:
- Negi A, Voisin-Chiret AS. Strategies to Reduce the On-Target Platelet Toxicity of Bcl-xL Inhibitors: PROTACs, SNIPERs and Prodrug-Based Approaches. Chembiochem. 2022 Mar 9:e202100689. doi: 10.1002/cbic.202100689. Epub ahead of print. PMID: 35263486.
Products are for research use only. Not for human use.
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