Free shipping on all orders over $ 500

DT2216

Cat. No. M10423
DT2216 Structure
Synonym:

DT-2216

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
Free Delivery on orders over USD 500 Bulk Inquiry?

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
References

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

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.

  Catalog
Abmole Inhibitor Catalog 2017




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

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.