Ribociclib
作者：齊岳
發布時間：2023-08-23
09:21:38
點擊數：
產品名稱：Ribociclib
產品描述：
| 產品描述 | LEE011 is an orally available, and highly specific CDK4/6 inhibitor (IC50：10/39 nM). |
| 靶點活性 | VEGFR6:39 nM, VEGFR4:10nM |
| 體外活性 | LEE011（200 mg/kg/day,p.o.）明顯延緩小鼠中BE2C 或者 1643細胞的生長,且無體重減輕或者其它的毒性癥狀. |
| 體內活性 | LEE011可抑制神經細胞瘤細胞的生長,該作用受到G1細胞周期阻滯和細胞衰老的調控。LEE011對17種神經細胞瘤中的12種均有顯著的生長抑制作用（平均IC50：307 nM）。 |
| 激酶實驗 | Enzyme assays are performed using a homogeneous time-resolved fluorescence assay with recombinant epitope tagged kinase domains (JAK1, 837-1142; JAK2, 828-1132; JAK3, 718-1124; Tyk2, 873-1187) or full-length enzyme (cMET and Chk2) and peptide substrate. Each enzyme reaction is performed with or without test compound (11-point dilution), JAK, cMET, or Chk2 enzyme, 500 nM (100 nM for Chk2) peptide, ATP (at the Km specific for each kinase or 1 mM), and 2.0% DMSO in assay buffer. The calculated IC50 value is the compound concentration required for inhibition of 50% of the fluorescent signal. Additional kinase assays are performed at Cerep using standard conditions at 200 nM. Enzymes tested included: Abl, Akt1, AurA, AurB, CDC2, CDK2, CDK4, CHK2, c-kit, EGFR, EphB4, ERK1, ERK2, FLT-1, HER2, IGF1R, IKKα, IKKβ, JNK1, Lck, MEK1, p38α, p70S6K, PKA, PKCα, Src, and ZAP70[1]. |
| 細胞實驗 | A panel of neuroblastoma cell lines, selected based upon prior demonstration of substrate adherent growth, is plated in triplicate on the Xcelligence Real-Time Cell Electronic Sensing system and treated 24 hours later with a four-log dose range of inhibitor or with a dimethyl sulfoxide (DMSO) control. Cell indexes are monitored continuously for ~100 hours, and IC50 values are determined as follows: growth curves are generated by plotting the cell index as a function of time and are normalized to the cell index at the time of treatment for a baseline cell index of 1. The area under the normalized growth curve from the time of treatment to 96 hours posttreatment is then calculated using a baseline area of 1 (the cell index at the time of treatment). Areas are normalized to the DMSO control, and the resulting data are analyzed using a nonlinear log inhibitor versus normalized response function. All experiments are repeated at least once. (Only for Reference) |
| 別名 | 瑞博西尼, LEE011 |
| 化合物與蛋白結合的復合物 |
The X-ray co-crystal structure of human CDK6 and Ribociclib. |
| 分子量 | 434.548 |
| 分子式 | C23H30N8O |
| CAS No. | 1211441-98-3 |
存儲
store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 7 mg/mL (16.1 mM)
H2O: <1 mg/mL
Ethanol: <1 mg/mL
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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