BETd-260

Product Name: BETd-260
CAS No.: 2093388-62-4
Chemical Name: BETd-260
Synonyms: ZBC260;BETd-260;BETd-260/ZBC260;9H-Pyrimido[4,5-b]indole-2-carboxamide, 4-[(3-cyclopropyl-1-ethyl-1H-pyrazol-5-yl)amino]-7-(3,5-dimethyl-4-isoxazolyl)-N-[5-[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1-oxo-1H-isoindol-4-yl]pentyl]-6-methoxy-;4-[(3-cyclopropyl-1-ethyl-1H-pyrazol-5-yl)amino]-7-(3,5-dimethyl-1,2-oxazol-4-yl)-N-{5-[2-(2,6-dioxopiperidin-3-yl)-1-oxo-2,3-dihydro-1H-isoindol-4-yl]pentyl}-6-methoxy-9H-pyrimido[4,5-b]indole-2-carboxamide
CBNumber: CB84667623
Molecular Formula: C43H46N10O6
Formula Weight: 798.89
MOL File: 2093388-62-4.mol

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BETd-260 Property

Density: 1.52±0.1 g/cm3(Predicted)
storage temp.: -80°C, protect from light, stored under nitrogen
solubility: DMSO : 25 mg/mL (31.29 mM);Water : < 0.1 mg/mL (insoluble)
form: Solid
pka: 10.73±0.40(Predicted)
color: Off-white to light yellow

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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.

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

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N-Bromosuccinimide Price

ChemScene

Product number: CS-0021622
Product name: BETd-260
Purity: 99.01%
Packaging: 5mg
Price: $450
Updated: 2021/12/16

ChemScene

Product number: CS-0021622
Product name: BETd-260
Purity: 99.01%
Packaging: 10mg
Price: $750
Updated: 2021/12/16

ChemScene

Product number: CS-0021622
Product name: BETd-260
Purity: 99.01%
Packaging: 25mg
Price: $1500
Updated: 2021/12/16

ChemScene

Product number: CS-0021622
Product name: BETd-260
Purity: 99.01%
Packaging: 50mg
Price: $2400
Updated: 2021/12/16

DC Chemicals

Product number: DC11566
Product name: BETd-260
Purity: >98%
Packaging: 100mg
Price: $1100
Updated: 2021/12/16

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BETd-260 Chemical Properties,Usage,Production

Description

BETd-260 is a PROTAC connected by ligands for Cereblon and BET. It potently suppresses cell viability and induces apoptosis in hepatocellular carcinomca (HCC) cells.

Uses

BETd-260 (ZBC 260) is a PROTAC connected by ligands for Cereblon and BET, with as low as 30 pM against BRD4 protein in RS4;11 leukemia cell line[1]. BETd-260 potently suppresses cell viability and robustly induces apoptosis in hepatocellular carcinoma (HCC) cells[2].

in vivo

BETd-260 (5 mg/kg, i.v., every other day, thrice a week for 3 weeks) causes rapid tumor regression with a maximum of >90% regression in mice bearing RS4;11 xenograft tumors, and with no body weight loss or other signs of toxicity in mice. BETd-260 (5 mg/kg, i.v.) degrades the BRD2, BRD3, and BRD4 proteins for more than 24 h, with robust cleavage of PARP and caspase-3, and strong down-regulation of c-Myc protein in RS4;11 xenograft mice model^[1].

IC 50

BRD4: <30 pM (IC₅₀); BRD2: 30-100 pM (IC₅₀); BRD3: 30-100 pM (IC₅₀)

References

[1] Zhou B, et al. Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. J Med Chem. 2018 Jan 25;61(2):462-481. DOI:10.1021/acs.jmedchem.6b01816
[2] Zhang H, et al. Targeting BET Proteins With a PROTAC Molecule Elicits Potent Anticancer Activity in HCC Cells. Front Oncol. 2020;9:1471. Published 2020 Jan 14. DOI:10.3389/fonc.2019.01471

BETd-260 Preparation Products And Raw materials

Raw materials

Preparation Products

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BETd-260 Suppliers

China 38 United States 3 Global 41

ShangHai Caerulum Pharma Discovery Co., Ltd.

Tel: 18149758185
Email: sales-cpd@caerulumpharma.com
Country: China
ProdList: 3506
Advantage: 58

Shanghai Lollane Biological Technology Co.,Ltd.

Tel: 021-52996696，15000506266 15000506266
Fax: +86-21-52996696
Country: China
ProdList: 4757
Advantage: 55

Chuzhou KeMail Chemical Technology Co., Ltd

Tel: 0550-5196001 15000891977
Fax: 0550-5196001
Email: wj520wjxby@126.com
Country: China
ProdList: 1944
Advantage: 55

Fan De(Beijing) Biotechnology Co., Ltd.

Tel: 15911056312
Email: liming@bio-fount.com
Country: China
ProdList: 9729
Advantage: 58

Jilin Province Woda Biotechnology Co., Ltd.

Tel: 13504435624
Email: 1927928688@qq.com
Country: China
ProdList: 1615
Advantage: 58

TargetMol Chemicals Inc.

Tel: +1-781-999-5354; +17819995354
Email: marketing@targetmol.com
Country: United States
ProdList: 32435
Advantage: 58

Zhejiang J&C Biological Technology Co.,Limited

Tel: +1-2135480471
Email: sales@sarms4muscle.com
Country: China
ProdList: 10473
Advantage: 58

Changzhou Chenhong Biotechnology Co., Ltd.

Tel: +86-0519-85788828 +86-13775037613
Email: sales@chemrenpharm.com
Country: China
ProdList: 3934
Advantage: 58

Shanghai hongqu biomedical technology co. LTD

Tel: 88888888888
Email: hongquchem@qq.com
Country: China
ProdList: 5132
Advantage: 58

ShangHai ChuanQian Chemcial Technique Centre

Tel: 15869524721
Email: 3525679403@qq.com
Country: China
ProdList: 4989
Advantage: 58

2093388-62-4, BETd-260Related Search:

BETd-260

ZBC260

9H-Pyrimido[4,5-b]indole-2-carboxamide, 4-[(3-cyclopropyl-1-ethyl-1H-pyrazol-5-yl)amino]-7-(3,5-dimethyl-4-isoxazolyl)-N-[5-[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1-oxo-1H-isoindol-4-yl]pentyl]-6-methoxy-

BETd-260/ZBC260

4-[(3-cyclopropyl-1-ethyl-1H-pyrazol-5-yl)amino]-7-(3,5-dimethyl-1,2-oxazol-4-yl)-N-{5-[2-(2,6-dioxopiperidin-3-yl)-1-oxo-2,3-dihydro-1H-isoindol-4-yl]pentyl}-6-methoxy-9H-pyrimido[4,5-b]indole-2-carboxamide

2093388-62-4

C43H46N10O6