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DT2216 | Degrader (PROTAC) of BCL2L1
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
BCL2L1
  • Ki:12.8 nM BCL-XL; 1.8 nM BCL-2; 300.9 nM BCL-W
  • DC50, Dmax, EC50:63 nM (DC50); 90.8% (Dmax); 52 nM (EC50)
Degrader (PROTAC)
100-500 nM, maximum 1 uM
1 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
No changes in BCL-2 levels in all cells examined. In addition, DT2216 had no effect on the levels ...
In Cell Selectivity Assessment
Selectivity Assessment Description:
Proteomics shows that DT2216 does not degrade any other protein.

Potency
Cellular
In Vitro

BCL2L1

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? No

In Vivo Validations

Mouse
Dose: 7.5-15 mg/Kg
Route of delivery: Intravenous
Plasma half life: 6.3 (IP), 6.1 (IV) h
Systemic clearance: 0.42 ml/min/Kg

Reference: --

Negative Control Compounds

DT2216NC

Orthogonal Probes def

A-1155463
WEHI-539
A-1331852

Chemical Information

Molecular Formula C77H96ClF3N10O10S4
SMILEs Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCC(=O)N2CCN(CC[C@H](CSc3ccccc3)Nc3ccc(S(=O)(=O)NC(=O)c4ccc(N5CCN(CC6=C(c7ccc(Cl)cc7)CCC(C)(C)C6)CC5)cc4)cc3S(=O)(=O)C(F)(F)F)CC2)C(C)(C)C)cc1
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
Molecular weight 1540.58 Da
AlogP 0.0
HBond acceptors 20
HBond donors 5
Atoms 201

References

Publications

Cross References

canSARChEMBL

Vendors

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Expert Reviews

by SERP
(on 19 Jan 2021)
Cellular Use Rating
In Model Organisms
It would be very useful to have information regarding the inhibition and degradation off-target profiling.
by SERP
(on 27 Jan 2021)
Cellular Use Rating
In Model Organisms
DT2216 is a proteolysis-targeting chimera (PROTAC) based on the BH3-mimetic ABT263 which targets BCLXL to the Von Hippel-Lindau (VHL) E3 ligase for degradation. Unlike ABT263 (which functionally inhibits...
by SERP
(on 8 Feb 2021)
Cellular Use Rating
In Model Organisms
DT2216 and its control substance DT2216NC represent a very good substance pair for investigating the role of BCL-XL degradation in both cells and animals. The authors present extensive evidence to support...
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