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Synonyms | LY2835219 mesylate | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C27H32F2N8.CH4O3S |
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分子量 | 602.7 | CAS No. | 1231930-82-7 | |
Solubility (25°C)* | 体外 | Water | 100 mg/mL (165.92 mM) | |
DMSO | 33 mg/mL (54.75 mM) | |||
Ethanol | 4 mg/mL (6.63 mM) | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | Abemaciclib mesylate is a potent and selective inhibitor of CDK4 and CDK6 with IC50 of 2 nM and 10 nM in cell-free assays, respectively. Phase 3. |
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in vitro | LY2835219 is an orally available cyclin-dependent kinase (CDK) inhibitor that targets the CDK4 (cyclin D1) and CDK6 (cyclin D3) cell cycle pathway, with potential antineoplastic activity. LY2835219 specifically inhibits CDK4 and 6, thereby inhibiting retinoblastoma (Rb) protein phosphorylation in early G1. Inhibition of Rb phosphorylation prevents CDK-mediated G1-S phase transition, thereby arresting the cell cycle in the G1 phase, suppressing DNA synthesis and inhibiting cancer cell growth. Overexpression of the serine/threonine kinases CDK4/6, as seen in certain types of cancer, causes cell cycle deregulation. [1] |
in vivo | LY2835219 saturates BBB efflux with an unbound plasma IC50 of about 95 nM. The percent of dose in brain for LY2835219-MsOH is 0.5–3.9%. In both a subcutaneous and intracranial human glioblastoma model (U87MG), LY2835219-MsOH suppressed tumor growth in a dose-dependent manner both as a single agent, and in combination with temozolomide. [1] |
細胞アッセイ | 細胞株 | SYO-1 cells |
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濃度 | 100 nM | |
反応時間 | 24 h | |
実験の流れ | Cells were cultured overnight and, on the next day (day 1), the media was replaced containing 100nM Abemaciclib or vehicle control (DMSO). |
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動物実験 | 動物モデル | Female C57BL/6 mice |
投薬量 | 50 mg/kg | |
投与方法 | i.p. |
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Data from [Biochem J, 2014, 459(3), 513-24]
Data from [Data independently produced by , , Cell Death Dis, 2018, 9(9):918]
Intracellular calcium links milk stasis to lysosome-dependent cell death during early mammary gland involution [ Cell Mol Life Sci, 2024, 81(1):29] | PubMed: 38212474 |
mTORC1 activity oscillates throughout the cell cycle promoting mitotic entry and differentially influencing autophagy induction [ bioRxiv, 2024, 2024.02.06.579216] | PubMed: 38370755 |
cGAS-STING drives ageing-related inflammation and neurodegeneration [ Nature, 2023, 620(7973):374-380] | PubMed: 37532932 |
Cyclin E-induced replicative stress drives p53-dependent whole-genome duplication [ Cell, 2023, 186(3):528-542.e14] | PubMed: 36681079 |
Inhibition of CDK4/6 regulates AD pathology, neuroinflammation and cognitive function through DYRK1A/STAT3 signaling [ Pharmacol Res, 2023, 190:106725] | PubMed: 36907286 |
Sequential activation of E2F via Rb degradation and c-Myc drives resistance to CDK4/6 inhibitors in breast cancer [ Cell Rep, 2023, 42(11):113198] | PubMed: 37865915 |
CDK4/6 inhibitors induce replication stress to cause long-term cell cycle withdrawal [ EMBO J, 2022, 10.15252/embj.2021108599] | PubMed: 35037284 |
Clinically relevant CHK1 inhibitors abrogate wild-type and Y537S mutant ERα expression and proliferation in luminal primary and metastatic breast cancer cells [ J Exp Clin Cancer Res, 2022, 41(1):141] | PubMed: 35418303 |
Overexpressed Cyclin D1 and CDK4 proteins are responsible for the resistance to CDK4/6 inhibitor in breast cancer that can be reversed by PI3K/mTOR inhibitors [ Sci China Life Sci, 2022, 10.1007/s11427-021-2140-8] | PubMed: 35982377 |
Implementation of a combined CDK inhibition and arginine-deprivation approach to target arginine-auxotrophic glioblastoma multiforme cells [ Cell Death Dis, 2022, 13(6):555] | PubMed: 35717443 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
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