DT2216
- CAS No.
- 2365172-42-3
- Chemical Name:
- DT2216
- Synonyms
- DT2216;DT2216,DT-2216;TPCK-treated Trypsin;(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-(pheny;L-Prolinamide, N-[7-[4-[(3R)-3-[[4-[[[4-[4-[[2-(4-chlorophenyl)-5,5-dimethyl-1-cyclohexen-1-yl]methyl]-1-piperazinyl]benzoyl]amino]sulfonyl]-2-[(trifluoromethyl)sulfonyl]phenyl]amino]-4-(phenylthio)butyl]-1-piperazinyl]-1,7-dioxoheptyl]-3-methyl-L-valyl-4-hydroxy-N-[(1S)-1-[4-(4-methyl-5-thiazolyl)phenyl]ethyl]-, (4R)-;(2S,4R)-1-[(2S)-2-[[7-[4-[(3R)-3-[4-[[4-[4-[[2-(4-chlorophenyl)-5,5-dimethyl-cyclohexen-1-yl]methyl]piperazin-1-yl]benzoyl]sulfamoyl]-2-(trifluoromethylsulfonyl)anilino]-4-phenylsulfanyl-butyl]piperazin-1-yl]-7-oxo-heptanoyl]amino]-3,3-dimethyl-butanoyl]-4-hydroxy-N-[(1S)-1-[4-(4-methylthiazol-5-yl)phenyl]ethyl]pyrrolidine-2-carboxamide;(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
- CBNumber:
- CB07247428
- Molecular Formula:
- C77H96ClF3N10O10S4
- Molecular Weight:
- 1542.36
- MDL Number:
- MOL File:
- 2365172-42-3.mol
- MSDS File:
- SDS
- TDS File:
- TDS
| Density | 1.39±0.1 g/cm3(Predicted) |
|---|---|
| storage temp. | -10 to -25°C |
| solubility |
DMSO:20.0(Max Conc. mg/mL);12.97(Max Conc. mM) Ethanol:10.0(Max Conc. mg/mL);6.48(Max Conc. mM) |
| pka | 4.60±0.10(Predicted) |
| form | Solid |
| color | White to light yellow |
| InChIKey | PXVFFBGSTYQHRO-VQWHJCJWNA-N |
| FDA UNII | Y8JQ9V7JAJ |
| UNSPSC Code | 12352200 |
| NACRES | NA.21 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302-H315-H319-H335 |
| Precautionary statements | P261-P280-P301+P312-P302+P352-P305+P351+P338 |
| WGK Germany | WGK 3 |
| Storage Class | 11 - Combustible Solids |
DT2216 price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 37311 | DT2216 ≥98% | 2365172-42-3 | 1mg | $29 | 2026-04-30 | Buy |
| Cayman Chemical | 37311 | DT2216 ≥98% | 2365172-42-3 | 5mg | $106 | 2026-04-30 | Buy |
| Cayman Chemical | 37311 | DT2216 ≥98% | 2365172-42-3 | 10mg | $197 | 2026-04-30 | Buy |
| Cayman Chemical | 37311 | DT2216 ≥98% | 2365172-42-3 | 25mg | $422 | 2026-04-30 | Buy |
| Biosynth | QUD17242 | DT2216 | 2365172-42-3 | 0.5mg | $285.56 | 2026-06-04 | Buy |
DT2216 Chemical Properties, Uses, Production
Uses
DT2216 is a potent and selective BCL-XL (Bcl-2 family member) degrader based on PROTAC technology. DT2216 causes effective degradation of BCL-XL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. DT2216 inhibits various BCL-XL-dependent leukemia and cancer cells but considerably less toxic to platelets. DT2216 is composed of the Bcl-2 family protein inhibitor Navitoclax (HY-10087), a linker, and a VHL E3 ubiquitin ligase (Red: Navitoclax; Blue: VHL ligand; Black: linker)[1].
Biological Activity
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.
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. |
IC 50
VHL
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. DOI:10.1038/s41591-019-0668-z
DT2216 Preparation Products And Raw materials
Raw materials
Preparation Products
DT2216 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Zhengzhou convergence chemical co., LTD | 037155153829 18003835034 | 3897192574@qq.com | China | 9982 | 58 |
| Nanjing Chemlin Chemical Co., Ltd | 025-83697070 13770331960 | info@chemlin.com.cn | China | 16305 | 64 |
| Shanghai Aladdin Bio-Chem Technology Co.,LTD | 400-6206333 13167063860 | anhua.mao@aladdin-e.com | China | 29977 | 65 |
| Sichuan Wei Keqi Biological Technology Co., Ltd. | 028-81700200 18116577057 | 3003855609@qq.com | China | 7717 | 56 |
| Shanghai Lollane Biological Technology Co.,Ltd. | 021-52996696，15000506266 15000506266 | China | 4859 | 55 | |
| ShangHai Angti Biotechnology Co., Ltd. | 13764913901 | info@angtibio.com | China | 4975 | 55 |
| Shanghai YuanYe Biotechnology Co., Ltd. | 15026964105 | 2881489226@qq.com | China | 89667 | 60 |
| ShangHai Biochempartner Co.,Ltd | 177-54423994 17754423994 | 2853530910@QQ.com | China | 8000 | 62 |
| Shanghai Rechem science Co., Ltd. | 021-31433387 15618786686 | sales@rechemscience.com | China | 2969 | 58 |
| Jilin Province Woda Biotechnology Co., Ltd. | 13504435624 | 1927928688@qq.com | China | 1644 | 58 |
