SML0666

GSK1210151A

≥98% (HPLC)

• Sinonimo/i: 7-(3,5-Dimethyl-4-isoxazolyl)-8-(methyloxy)-1-[(1R)-1-(2-pyridinyl)ethyl]-1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-one, I-BET151
• Formula empirica (notazione di Hill): C₂₃H₂₁N₅O₃
• Numero CAS: 1300031-49-5
• Peso molecolare: 415.44
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Saggio: ≥98% (HPLC)
• Forma fisica: powder
• Colore: white to beige
• Solubilità: DMSO: 20 mg/mL, clear
• Ideatore: GlaxoSmithKline
• Malattie correlate: cancer
• Temperatura di conservazione: 2-8°C
• InChI: 1S/C23H21N5O3/c1-12-21(14(3)31-27-12)16-9-18-15(10-20(16)30-4)22-19(11-25-18)26-23(29)28(22)13(2)17-7-5-6-8-24-17/h5-11,13H,1-4H3,(H,26,29)/t13-/m1/s1; VUVUVNZRUGEAHB-CYBMUJFWSA-N

Descrizione

Applicazioni

GSK1210151A or I-BET151 has been used to study its inhibitory effect on BET (bromodomain and extra terminal) recruitment to chromatin in treating MLL (mixed-lineage leukemia)-fusion leukemia.

Azioni biochim/fisiol

GSK1210151A (I-BET151) is an inhibitor of the BET (bromodomain and extra terminal domain protein) family of acetyl-lysine recognizing, chromatin ′adaptor′ proteins. GSK1210151A displaces BRD3 and BRD4, PAFc and SEC components from chromatin resulting in inhibition of transcription at key genes (BCL2, C-MYC and CDK6) involved in the initiation of mixed lineage leukemia (MLL). GSK1210151A (I-BET151) showed good efficacy in 2 MLL animal models.

Altre note

GSK1210151A has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the GSK1210151A probe summary on the Chemical Probes Portal website.

Informazioni sulla sicurezza

• Pittogrammi: GHS06
• Avvertenze: Danger
• Indicazioni di pericolo: H301
• Consigli di prudenza: P264 - P270 - P301 + P310 - P405 - P501
• Classi di pericolo: Acute Tox. 3 Oral
• Codice della classe di stoccaggio: 6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable