DT2216 | BCL-XL PROTAC Degrader |CAS 2365172-42-3| DC Chemicals

Cas No.:	2365172-42-3
Chemical Name:	DT-2216
Synonyms:	DT2216;DT-2216;DT 2216
SMILES:	CC1(CC(CN2CCN(C3C=CC(C(=O)NS(=O)(C4C=CC(N[C@H](CCN5CCN(C(=O)CCCCCC(=O)N[C@H](C(=O)N6C[C@H](O)C[C@H]6C(=O)N[C@@H](C)C6C=CC(C7SC=NC=7C)=CC=6)C(C)(C)C)CC5)CSC5C=CC=CC=5)=C(S(=O)(=O)C(F)(F)F)C=4)=O)=CC=3)CC2)=C(C2C=CC(Cl)=CC=2)CC1)C
Formula:	C₇₇H₉₆ClF₃N₁₀O₁₀S₄
M.Wt:	1542.36
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:	[1]. Khan S, et al. A selective BCL-XL PROTAC degrader achieves safe and potent antitumor activity. Nat Med. 2019 Dec;25(12):1938-1947.

Description:	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[1].
Target:	VHL
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[1]. Animal Model: CB17/Icr-Prkdcscid/IcrIcoCrl (CB-17 SCID) mice aged 5-6 weeks[1] Dosage: 7.5, 15 mg/kg Administration: i.p.; weekly for 60 days Result: Suppressed the growth of MOLT-4 T-ALL xenografts in mice.
In Vitro:	DT2216 (62.5, 125 nM; 72 hours) kills MOLT-4 cells[1]. ABT263 (0.001-10 μM; 72 hour) shows highly toxic to MOLT-4 cells with an EC50 of 0.052 μM[1]. 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[1]. Apoptosis Analysis[1] Cell Line: MOLT-4 cells Concentration: 62.5, 125 nM Incubation Time: 72 hours Result: Killed MOLT-4 cells. Cell Cytotoxicity Assay[1] Cell Line: MOLT-4 cells Concentration: 0.001, 0.01, 0.1, 1, 10 μM Incubation Time: 72 hours Result: Showed highly toxic to MOLT-4 cells with an EC50 of 0.052 μM. Western Blot Analysis[1] Cell Line: MOLT-4 cells Concentration: 0.1, 0.3 μM Incubation Time: 24 hours Result: Killed 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.
References:	[1]. Khan S, et al. A selective BCL-XL PROTAC degrader achieves safe and potent antitumor activity. Nat Med. 2019 Dec;25(12):1938-1947.

Cat. No.	Product name	Field of application
DC65211	KT-474	KT-474 is a highly active and selective, orally bioavailable IRAK4 degrader being developed for the treatment of toll-like receptor (TLR)/interleukin-1 receptor (IL-1R)-driven immune-inflammatory diseases.
DC39826	Homo-PROTAC cereblon degrader 1	Homo-PROTAC cereblon degrader 1, is a cereblon degrader.
DC74523	XY-07-35	XY-07-35 is a potent, selective HDAC6 proteolysis targeting chimera (PROTAC) degrader with IC50 of 48.5 nM.
DC74496	HJM-561	HJM-561 is a potent, selective and orally bioavailable EGFR PROTAC degrader, selectively degrades the EGFR C797S-containing triple mutants Del19/T790M/C797S and L858R/T790M/C797S with DC50 values of 9.2 nM and 5.8 nM, respectively.
DC74494	GNE-0011	GNE-0011 is a monovalent, JQ1-based BRD4 degrader that is not linked to an E3 ligase binder, triggers proteasomal and ubiquitin-dependent selective degradation of BRD4 over BRD2 and BRD3.
DC74479	BSJ-05-037	BSJ-05-037 is a potent and selective heterobifunctional degrader of ITK with DC50 of 17.6-41.8 nM in TCL lines DERL-2 and Hut78.
DC72756	JQAD1	JQAD1 is a CRBN-dependent PROTAC that selectively targets EP300 for degradation. JQAD1 suppresses EP300 expression and the H3K27ac modification. JQAD1 induces apoptosis. JQAD1 can be used in research of cancer.
DC50038	PROTAC SGK3 degrader-1	PROTAC SGK3 degrader-1 (SGK3-PROTAC1), is a potent SKG3 degrader based on PROTAC. PROTAC SGK3 degrader-1 (0.3 μM) induces 50% degradation of endogenous SGK3 within 2 hours, with maximal 80% degradation observed within 8 hours, accompanied by a loss of phosphorylation of NDRG1 (an SGK3 substrate).
DC48434	TD-165	TD165(TD 165) is a PROTAC-based cereblon (CRBN) degrader that degrads Cav1.2α with the DC50 of 20.4 nM, comprising a cereblon (CRBN) ligand binding group, a linker and an von Hippel-Landau (VHL) binding group.
DC46405	ARD-2128	ARD2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity. ARD-2128 has the potential for the research of the prostate cancer.