2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-(4-(2-pyridyl)benzyl)-9-isopropylpurinetrihydrochloride

Product Name: 2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-(4-(2-pyridyl)benzyl)-9-isopropylpurinetrihydrochloride
CAS No.: 294646-77-8
Chemical Name: 2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-(4-(2-pyridyl)benzyl)-9-isopropylpurinetrihydrochloride
Synonyms: R8;(S)-CR8;(R)-CR8;CR8 3HCl (R);CR8, (R)-Isomer;(R)?-?CR8/CR8/(R)-Isomer;(R)-CR8|||(R)-Isomer|||CR8;CR8, (R)-Isomer - CAS 294646-77-8 - Calbiochem;(R)-2-((9-Isopropyl-6-((4-(pyridin-2-yl)benzyl)amino)-9H-purin-2-yl)amino)butan-1-ol;(R)-2-(1-Hydroxybut-2-ylamino)-6-[4-(2-pyridyl)phenylmethylamino]-9-iso-propylpurine
CBNumber: CB32518863
Molecular Formula: C24H29N7O
Formula Weight: 431.53
MOL File: 294646-77-8.mol

More

Less

2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-(4-(2-pyridyl)benzyl)-9-isopropylpurinetrihydrochloride Property

Melting point:: 98-100℃
Boiling point:: 671.4±65.0 °C(Predicted)
Density: 1.27±0.1 g/cm3(Predicted)
storage temp.: 2-8°C
solubility: DMSO: ≥10mg/mL
form: powder
pka: 14.56±0.10(Predicted)
color: off-white
Stability:: Stable for 2 years as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.

More

Less

Safety

Hazard Codes: Xn
Risk Statements: 22
WGK Germany: 3

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.

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

More

Less

N-Bromosuccinimide Price

Sigma-Aldrich

Product number: C3249
Product name: CR8
Purity: ≥95% (HPLC)
Packaging: 5mg
Price: $131.2
Updated: 2024/03/01

Sigma-Aldrich

Product number: C3249
Product name: CR8
Purity: ≥95% (HPLC)
Packaging: 25mg
Price: $524
Updated: 2024/03/01

Cayman Chemical

Product number: 14006
Product name: (R)-CR8
Purity: ≥98%
Packaging: 1mg
Price: $57
Updated: 2024/03/01

Cayman Chemical

Product number: 14006
Product name: (R)-CR8
Purity: ≥98%
Packaging: 10mg
Price: $275
Updated: 2024/03/01

Cayman Chemical

Product number: 14006
Product name: (R)-CR8
Packaging: 5mg
Price: $179
Updated: 2024/03/01

More

Less

2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-(4-(2-pyridyl)benzyl)-9-isopropylpurinetrihydrochloride Chemical Properties,Usage,Production

Description

CR8 (294646-77-8) is a second generation analog of roscovitine which inhibits cyclin-dependent kinases with increased potency, Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, Cdk5, p25, and Cdk9/cyclin T, IC50s=0.09, 0.072, 0.041, 0.11 and 0.18 μM respectively.1,2 Acts as a molecular glue degrader that depletes cyclin K.3 CR8 displays neuroprotective effects in various models including traumatic brain injury.4

Uses

CR8, (R)-Isomer is a cell-permeable, ATP-binding pocket-targeting CDK/CK1 dual-specific inhibitor.

Biochem/physiol Actions

CR8 is a potent and selective inhibitor of cyclin dependent kinase (CDK1, 2, 5, 7, and 9). CR8 is a more potent pyridyl analogue of roscovitine (Cat. No. R7772). In comparison to roscovirtine, the compound gains in potency toward CK1, which is involved in amyloid-β formation. The R-CR8 enantiomer is slightly more potent than S. CR8 is around 30 times more potent at cellular assay then roscovitine. Acts as a molecular glue to induce cyclin K degradation.

References

Bettayeb et al. (2008), C8, a potent and selective, roscovitine-derived inhibitor of cyclin-dependent kinases; Oncogene, 27 5797 Bettayeb et al. (2010), CDK Inhibitors Roscovitine and CR8 Trigger Mcl-1 Down-Regulation and Apoptotic Cell Death in Neuroblastoma Cells; Genes Cancer, 1 369 Slabiki et al. (2020), The CDK inhibitor CR8 acts as a molecular glue degrader that depletes cyclin K; Nature, 585 293 Aubrecht et al. (2018), Comparing effects of CDK inhibitor and E2F1/2 ablation on neuronal cell death pathways in vitro and after traumatic brain injury; Cell Death Dis., 9 112

2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-(4-(2-pyridyl)benzyl)-9-isopropylpurinetrihydrochloride Preparation Products And Raw materials

Raw materials

Preparation Products

More

Less

2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-(4-(2-pyridyl)benzyl)-9-isopropylpurinetrihydrochloride Suppliers

China 59 United Kingdom 1 United States 9 Global 69

3B Pharmachem (Wuhan) International Co.,Ltd.

Tel: 821-50328103-801 18930552037
Fax: 86-21-50328109
Email: 3bsc@sina.com
Country: China
ProdList: 15839
Advantage: 69

Bide Pharmatech Ltd.

Tel: 400-164-7117 13681763483
Fax: +86-21-61629029
Email: product02@bidepharm.com
Country: China
ProdList: 41462
Advantage: 60

Sigma-Aldrich

Tel: 021-61415566 800-8193336
Email: orderCN@merckgroup.com
Country: China
ProdList: 51456
Advantage: 80

Shanghaizehan biopharma technology co., Ltd.

Tel: 021-61350663 13052117465
Fax: 021-61350662
Email: sales@zehanbiopharma.com
Country: China
ProdList: 1004
Advantage: 55

EMMX Biotechnology LLC

Tel: 888-539-0666
Fax: 888-539-0666
Email: info@emmx.com
Country: United States
ProdList: 8447
Advantage: 60

Shanghai EFE Biological Technology Co., Ltd.

Tel: 021-65675885 18964387627
Fax: 021-65675885
Email: info@efebio.com
Country: China
ProdList: 9806
Advantage: 58

Shanghai YuanYe Biotechnology Co., Ltd.

Tel: 021-61312847; 18021002903
Fax: QQ:3008007432
Email: 3008007409@qq.com
Country: China
ProdList: 27313
Advantage: 60

ShangHai Biochempartner Co.,Ltd

Tel: 177-54423994 17754423994
Fax: QQ:2853530913
Email: 2853530910@QQ.com
Country: China
ProdList: 8010
Advantage: 62

Shanghai Rechem science Co., Ltd.

Tel: 21-31433387 15618786686
Fax: QQ:1369748377
Email: sales@rechemscience.com
Country: China
ProdList: 2987
Advantage: 58

Shanghai Chaolan Chemical Technology Center

Tel: 021-QQ：65489617 15618227136
Fax: 21-5161 9052
Email: Sales@ATKchemical.com
Country: China
ProdList: 7295
Advantage: 58

294646-77-8, 2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-(4-(2-pyridyl)benzyl)-9-isopropylpurinetrihydrochlorideRelated Search:

3-[(Aminocarbonyl)amino]-5-(3-fluorophenyl)-N-(3S)-3-piperidinyl-2-Thiophenecarboxamide METHOPRENE ACID Fruquintinib|HMPL-013 Volasertib (BI 6727) Cumene 3-Methyl-2-butanone 2-Chloropropane 2-Bromopropane

(R)-CR8

2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-(4-(2-pyridyl)benzyl)-9-isopropylpurinetrihydrochloride

1-Butanol,2-[[9-(1-Methylethyl)-6-[[[4-(2-pyridinyl)phenyl]Methyl]aMino]-9H-purin-2-yl]aMino]-,(2R)-

(S)-CR8

(2R)-2-[[9-(1-Methylethyl)-6-[[[4-(2-pyridinyl)phenyl]methyl]amino]-9H-purin-2-yl]amino]-1-butanol

R8

CR8, (R)-Isomer

(2R)-2-[[9-(1-Methylethyl)-6-[[[4-(2-pyridinyl)phenyl]methyl]amino]-9H-purin-2-yl]amino]-butanol-1

(R)-2-(1-Hydroxybut-2-ylamino)-6-[4-(2-pyridyl)phenylmethylamino]-9-iso-propylpurine

CR8, (R)-Isomer - CAS 294646-77-8 - Calbiochem

(R)-2-((9-Isopropyl-6-((4-(pyridin-2-yl)benzyl)amino)-9H-purin-2-yl)amino)butan-1-ol

CR8 3HCl (R)

Inhibitor,(R)??CR8,caspases,Cyclin dependent kinase,lesion,death,inhibit,cell,(R)?-?CR-8,CDK,CR8, (R)-Isomer,(R)?-?CR8,(R)? ?CR8,Hippocampus,neuroprotective,Apoptosis,PARP

(R)?-?CR8/CR8/(R)-Isomer

(R)-CR8|||(R)-Isomer|||CR8

294646-77-8

C24H29N7O3HCl