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别名 | LY2835219 mesylate | 储存条件 (自收到货起) |
3年 / -20°C / 粉状 1年 / -80°C / 溶于溶剂 |
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化学式 | C27H32F2N8.CH4O3S |
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分子量 | 602.7 | CAS号 | 1231930-82-7 | |
Solubility (25°C)* | 体外 | Water | 100 mg/mL (165.92 mM) | |
Ethanol | 100 mg/mL (165.92 mM) | |||
DMSO warmed with 50ºC water bath | 33 mg/mL (54.75 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. |
产品描述 | Abemaciclib mesylate是一种有效的,选择性CDK4和CDK6抑制剂,无细胞试验中IC50分别为2 nM和10 nM。Phase 3。 | ||||
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体外研究 | LY2835219是一种口服有效的细胞周期蛋白依赖性激酶(CDK)抑制剂,靶向作用于CDK4(cyclin D1)和CDK6(cyclin D3)细胞周期通路,具有潜在的抗肿瘤活性。LY2835219特异性抑制CDK4和6,从而在早G1期抑制视网膜母细胞瘤(Rb)蛋白磷酸化。抑制Rb磷酸化,防止CDK-介导的G1-S期转换,从而使细胞周期停滞在G1期,抑制DNA合成,且抑制癌细胞生长。某些类型的癌症中丝/苏氨酸激酶CDK4/6的过表达,导致细胞周期调节失控。[1] |
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体内研究 | LY2835219-MsOH处理脑的剂量百分比为0.5–3.9%。LY2835219-MsOH处理皮下和颅内胶质瘤模型(U87MG),抑制肿瘤生长,这种作用存在剂量依赖性,不管是单独处理,还是与Temozolomide联用。[1] |
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数据来源于[, 459(3), 513-24]
数据来源于[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 |
特定的存储和包装每个产品的信息在产品说明书上都有注明。大多数Selleck产品,在推荐的条件下存储可稳定保存两年。产品有时建议的储存温度不同,大多数建议储存在-20°C,抑制剂属于化学试剂,可在常温下运输储存两周左右。即使如此,我们保证产品的出货量将保持产品质量的条件下,一般都会放入冰袋。望阁下收到产品后,请按照产品数据表建议适当存储。
如果需要长期保存,请于零下二十度低温保存。禁止用于人体及治疗!
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