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;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;2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-(4-(2-pyridyl)benzyl)-9-isopropylpurinetrihydrochloride
- CBNumber:
- CB32518863
- Molecular Formula:
- C24H29N7O
- Molecular Weight:
- 431.53
- MDL Number:
- MFCD18785641
- MOL File:
- 294646-77-8.mol
- MSDS File:
- SDS
2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-(4-(2-pyridyl)benzyl)-9-isopropylpurinetrihydrochloride Properties
| 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 |
| pka | 14.56±0.10(Predicted) |
| form | powder |
| color | off-white |
| Stability | Stable for 2 years as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month. |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H302-H315-H319-H335 | |||||||||
| Precautionary statements | P261-P305+P351+P338 | |||||||||
| Hazard Codes | Xn | |||||||||
| Risk Statements | 22 | |||||||||
| WGK Germany | 3 | |||||||||
| NFPA 704 |
|
2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-(4-(2-pyridyl)benzyl)-9-isopropylpurinetrihydrochloride price More Price(14)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | C3249 | CR8 ≥95% (HPLC) | 294646-77-8 | 5mg | $131.2 | 2024-03-01 | Buy |
| Sigma-Aldrich | C3249 | CR8 ≥95% (HPLC) | 294646-77-8 | 25mg | $524 | 2024-03-01 | Buy |
| Cayman Chemical | 14006 | (R)-CR8 ≥98% | 294646-77-8 | 1mg | $57 | 2024-03-01 | Buy |
| Cayman Chemical | 14006 | (R)-CR8 ≥98% | 294646-77-8 | 10mg | $275 | 2024-03-01 | Buy |
| Cayman Chemical | 14006 | (R)-CR8 | 294646-77-8 | 5mg | $179 | 2024-03-01 | Buy |
2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-(4-(2-pyridyl)benzyl)-9-isopropylpurinetrihydrochloride Chemical Properties,Uses,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
2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-(4-(2-pyridyl)benzyl)-9-isopropylpurinetrihydrochloride Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32480 | 60 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
| Career Henan Chemica Co | +86-0371-86658258 15093356674; | laboratory@coreychem.com | China | 30255 | 58 |
| 3B Pharmachem (Wuhan) International Co.,Ltd. | 821-50328103-801 18930552037 | 3bsc@sina.com | China | 15848 | 69 |
| Bide Pharmatech Ltd. | 400-1647117 15221909166 | product02@bidepharm.com | China | 41438 | 60 |
| Sigma-Aldrich | 021-61415566 800-8193336 | orderCN@merckgroup.com | China | 51471 | 80 |
| EMMX Biotechnology LLC | 888-539-0666 | info@emmx.com | United States | 8449 | 60 |
| Shanghai EFE Biological Technology Co., Ltd. | 021-65675885 18964387627 | info@efebio.com | China | 9709 | 58 |
| Shanghai YuanYe Biotechnology Co., Ltd. | 021-61312847; 18021002903 | 3008007409@qq.com | China | 27322 | 60 |
| ShangHai Biochempartner Co.,Ltd | 17754423994 17754423994 | 2853530910@QQ.com | China | 8018 | 62 |