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SML3522

Sigma-Aldrich

DT2216

≥90% (HPLC)

Synonym(s):

(2S,4R)-1-((S)-2-(7-(4-((R)-3-((4-(N-(4-(4-((4′-chloro-4,4-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazin-1-yl)benzoyl)sulfamoyl)-2-((trifluoromethyl)sulfonyl)phenyl)amino)-4-(phenylthio)butyl)piperazin-1-yl)-7-oxoheptanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide, DT 2216, DT-2216

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About This Item

Empirical Formula (Hill Notation):
C77H96ClF3N10O10S4
CAS Number:
2365172-42-3
Molecular Weight:
1542.36
UNSPSC Code:
12352200
NACRES:
NA.21

Quality Level

100

Assay

≥90% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear (Warmed)

storage temp.

-10 to -25°C

SMILES string

CC(C)(C1)CCC(C2=CC=C(C=C2)Cl)=C1CN3CCN(C4=CC=C(C=C4)C(NS(=O)(C5=CC(S(C(F)(F)F)(=O)=O)=C(C=C5)N[C@@H](CSC6=CC=CC=C6)CCN7CCN(CC7)C(CCCCCC(N[C@@H](C(C)(C)C)C(N8[C@@H](C[C@H](C8)O)C(N[C@H](C9=CC=C(C%10=C(N=CS%10)C)C=C9)C)=O)=O)=O)=O)=O)=O)CC3

Biochem/physiol Actions

DT2216 is a selective BCL-XL, but not BCL-2 or BCL-W, degrader composed of a von Hippel-Lindau (VHL) E3 ligase-targeting ligand linked to a ABT-263 (navitoclax) derivative. DT2216 is more potent than ABT-263 against BCL-XL-dependent leukemia (MOLT-4 IC50 = 52 vs 191 nM) and cancer cells (MDA-MB-231 IC50 = 229 vs 707 nM). DT2216 effectively inhibits the growth of several xenograft tumors in vivo either alone (15 mg/kg/wk i.p.) or in combination with other chemotherapeutic agents (docetaxel or VDL), exhbiting improved efficacy and reduced thrombocytopenia when compared with ABT-263 as a result of greatly reduced platelet toxicity due to poor VHL expression in platelets.

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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BCL-XL PROTAC degrader DT2216 synergizes with sotorasib in preclinical models of KRASG12C-mutated cancers
Sajid Khan
Journal of Hematology & Oncology, 15, 23-23 (2022)
Overcoming Gemcitabine Resistance in Pancreatic Cancer Using the BCL-XL-Specific Degrader DT2216
Dinesh Thummuri, Sajid Khan, Janet Wiegand
Molecular Cancer Therapeutics, 21, 184-192 (2022)
Ryan Kolb et al.
Nature communications, 12(1), 1281-1281 (2021-02-26)
Regulatory T cells (Tregs) play an important role in maintaining immune homeostasis and, within tumors, their upregulation is common and promotes an immunosuppressive microenvironment. Therapeutic strategies that can eliminate Tregs in the tumor (i.e., therapies that do not run the
Yonghan He et al.
Journal of hematology & oncology, 13(1), 95-95 (2020-07-18)
Patients with advanced T cell lymphomas (TCLs) have limited therapeutic options and poor outcomes in part because their TCLs evade apoptosis through upregulation of anti-apoptotic Bcl-2 proteins. Subsets of TCL cell lines, patient-derived xenografts (PDXs), and primary patient samples depend
Sajid Khan et al.
Nature medicine, 25(12), 1938-1947 (2019-12-04)
B-cell lymphoma extra large (BCL-XL) is a well-validated cancer target. However, the on-target and dose-limiting thrombocytopenia limits the use of BCL-XL inhibitors, such as ABT263, as safe and effective anticancer agents. To reduce the toxicity of ABT263, we converted it

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