DT2216 is a selective B-cell lymphoma extra large (BCL-XL) proteolysis-targeting chimera (PROTAC). DT2216 targets BCL-XL to the Von Hippel-Lindau (VHL) E3 ligase for degradation. DT2216 inhibits various BCL-XL-dependent leukemia and cancer cells but considerably less toxic to platelets.
In vivo, DT2216 (i.p.; 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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO 20 mg/mL|
The PROTAC DT2216 Targets Cancer by Promoting BCL-X L Degradation
Cancer Discov. 2020 Feb;10(2):174. PMID: 34365411.
DT2216-a Bcl-xL-specific degrader is highly active against Bcl-xL-dependent T cell lymphomas
Yonghan He, et al. J Hematol Oncol. 2020 Jul 16;13(1):95. PMID: 32677976.
A selective BCL-X L PROTAC degrader achieves safe and potent antitumor activity
Sajid Khan, et al. Nat Med. 2019 Dec;25(12):1938-1947. PMID: 31792461.
|Related PROTAC Products|
MT-802 is a potent BTK degrader based on PROTAC technology, it induces Bruton's tyrosine kinase (BTK) knockdown.
|PROTAC KRASG12C Degrader-LC-2
PROTAC KRASG12C Degrader-LC-2 is a potent first-in-class PROTAC capable of degrading endogenous KRAS G12C, with DC50s between 0.25 and 0.76 μM.
|Homo-PROTAC pVHL30 degrader 1
Homo-PROTAC pVHL30 degrader 1 is a pVHL30 degrader based on PROTAC and a potent VHL inhibitor.
|Homo-PROTAC cereblon degrader 1 (OUN20985)
Homo-PROTAC cereblon degrader 1 (OUN20985) is a potent and efficient cereblon (CRBN) degrader with minimal effects on IKZF1 and IKZF3.
|PROTAC SGK3 degrader-1
PROTAC SGK3 degrader-1 (SGK3-PROTAC1) is a potent SGK3 degrader, it is a PROTAC conjugate of the 308-R SGK inhibitor with the VH032 VHL binding ligand, targeting SGK3.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.