DT2216

Product Name: DT2216
CAS No.: 2365172-42-3
Chemical Name: DT2216
Synonyms: DT2216;DT2216,DT-2216;(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
Formula Weight: 1542.36
MOL File: 2365172-42-3.mol

More

Less

DT2216 Property

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

More

Less

Safety

WGK Germany: WGK 3
Storage Class: 11 - Combustible Solids

More

Less

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

More

Less

DT2216 Chemical Properties,Usage,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

More

Less

DT2216 Suppliers

China 73 United States 1 Global 74

Zhengzhou convergence chemical co., LTD

Tel: 037155153829 18003835034
Email: 3897192574@qq.com
Country: China
ProdList: 9991
Advantage: 58

Wuhan Shanhai Zhihe Biotechnology Co., Ltd.

Tel: 17771424646
Email: shoubull@126.com
Country: China
ProdList: 944
Advantage: 58

Nanjing Chemlin Chemical Co., Ltd

Tel: 025-83697070 13913916777
Fax: +86-25-83453306
Email: info@chemlin.com.cn
Country: China
ProdList: 16053
Advantage: 64

Shanghai Aladdin Bio-Chem Technology Co.,LTD

Tel: 400-6206333 13167063860
Fax: 021-50323701
Email: anhua.mao@aladdin-e.com
Country: China
ProdList: 26647
Advantage: 65

Sichuan Wei Keqi Biological Technology Co., Ltd.

Tel: 028-81700200 18116577057
Fax: 028-81705658
Email: 3003855609@qq.com
Country: China
ProdList: 7777
Advantage: 56

Shanghai Lollane Biological Technology Co.,Ltd.

Tel: 021-52996696，15000506266 15000506266
Fax: +86-21-52996696
Country: China
ProdList: 4817
Advantage: 55

ShangHai Angti Biotechnology Co., Ltd.

Tel: 13764913901
Fax: -
Email: info@angtibio.com
Country: China
ProdList: 4974
Advantage: 55

Shanghai YuanYe Biotechnology Co., Ltd.

Tel: 021-61312847; 18021002903
Fax: QQ:3008007432
Email: 3008007409@qq.com
Country: China
ProdList: 86249
Advantage: 60

ShangHai Biochempartner Co.,Ltd

Tel: 177-54423994 17754423994
Fax: QQ:2853530913
Email: 2853530910@QQ.com
Country: China
ProdList: 7999
Advantage: 62

Shanghai Rechem science Co., Ltd.

Tel: 021-31433387 15618786686
Fax: QQ:1369748377
Email: sales@rechemscience.com
Country: China
ProdList: 2984
Advantage: 58

More

Less

View Lastest Price from DT2216 manufacturers

Hubei Chuchang Biotech Co., Ltd.

Product: DT2216 2365172-42-3
Price: US $0.00-0.00/MG
Min. Order: 1MG
Purity: 98
Supply Ability: 100G
Release date: 2024-04-17

2365172-42-3, DT2216Related Search:

DT2216

DT2216,DT-2216

(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

(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

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-((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

2365172-42-3

C77H96ClF3N10O10S4