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DT2216

Cat. No. M10423
DT2216 Structure
Synonym:

DT-2216

Size Price Availability Quantity
5mg USD 210  USD210 In stock
10mg USD 340  USD340 In stock
25mg USD 720  USD720 In stock
50mg USD 1080  USD1080 In stock
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Quality Control & Documentation
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.

Chemical Information
Molecular Weight 1542.36
Formula C77H96ClF3N10O10S4
CAS Number 2365172-42-3
Solubility (25°C) DMSO 20 mg/mL
Storage -20°C, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Cancer Discov. The PROTAC DT2216 Targets Cancer by Promoting BCL-X L Degradation

[2] Yonghan He, et al. J Hematol Oncol. DT2216-a Bcl-xL-specific degrader is highly active against Bcl-xL-dependent T cell lymphomas

[3] Sajid Khan, et al. Nat Med. A selective BCL-X L PROTAC degrader achieves safe and potent antitumor activity

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

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