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Cat. No. M10423
DT2216 Structure


Size Price Availability Quantity
5mg USD 189  USD210 In stock
10mg USD 306  USD340 In stock
25mg USD 648  USD720 In stock
50mg USD 972  USD1080 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 1542.36
Formula C77H96ClF3N10O10S4
CAS Number 2365172-42-3
Purity >98%
Solubility DMSO 20 mg/mL
Storage -20°C, sealed

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.

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Abmole Inhibitor Catalog 2017

Keywords: DT2216, DT-2216 supplier, PROTAC, inhibitors

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