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Abemaciclib (LY2835219) 是一种 CDK4/6 的双重抑制剂 (IC50=2/10 nM),具有选择性和特异性。Abemaciclib 具有抗肿瘤活性,被用于治疗晚期或转移性乳腺癌。

Abemaciclib (LY2835219) 是一种 CDK4/6 的双重抑制剂 (IC50=2/10 nM),具有选择性和特异性。Abemaciclib 具有抗肿瘤活性,被用于治疗晚期或转移性乳腺癌。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 198 | In stock | |
| 5 mg | ¥ 378 | In stock | |
| 10 mg | ¥ 546 | In stock | |
| 25 mg | ¥ 659 | In stock | |
| 50 mg | ¥ 993 | In stock | |
| 100 mg | ¥ 1,230 | In stock | |
| 200 mg | ¥ 1,560 | In stock | |
| 500 mg | ¥ 2,860 | In stock |
Abemaciclib 相关产品
| 产品描述 | Abemaciclib (LY2835219) is a dual inhibitor of CDK4/6 (IC50=2/10 nM) with selectivity and specificity. Abemaciclib has antitumor activity and is used to treat advanced or metastatic breast cancer. |
| 靶点活性 | FLT3:3960 nM, CDK5-p35:287 nM, CDK6:10 nM, CDK7:3910 nM, GSK-3β:192 nM, CDK5:355 nM, PIM2:3400 nM, CDK7-CyclinH-MAT1:3910 nM, CDK1-cyclinB1:1627 nM, CDK2:504 nM, DRAK1:659 nM, CDK1:1627 nM, CDK4:2 nM, JNK3:389 nM, CK2:117 nM, CDK5-p25:355 nM, HIPK2:31 nM, DYRK2:61 nM, CDK9-CyclinT1:57 nM, PIM1:50 nM, GSK3b:192 nM, FLT3 (D835Y):403 nM, CDK2-CyclinE:504 nM |
| 体外活性 | 方法:HNSCC 细胞系 OSC-19、FaDu 和 YD-10B 用 Abemaciclib (0.01-10 μM) 处理 72 h,使用 Cell Counting Kit 检测细胞活力。 |
| 体内活性 | 方法:为检测体内抗肿瘤活性,将 Abemaciclib (45-90 mg/kg in 1% HEC in 20 mM phosphate buffer (pH2.0)) 灌胃给药给携带人舌鳞癌肿瘤 OSC-19 的 BALB/c 小鼠,每天一次,持续十四天。 |
| 激酶实验 | Cells (5×103) are plated in 96 well plates. Cells are treated the next day for 24 to 48 hours and then assessed for caspase-3 activity by Caspase-Glo-3/7 Assay, as per manufacturer's instructions and a luminescence plate reader. |
| 细胞实验 | LY2835219 is dissolved in DMSO to a 10 mM concentration.? Cells are seeded in a 96-well plate, allowed to adhere overnight, and treated with DMSO control (0.1% v/v) or the indicated compounds for 72 h. Cell viability and proliferation are determined using a Cell Counting Kit according to the manufacturer's instructions. The interaction between LY2835219 and mTOR inhibitor is determined using CompuSyn. Combination index (CI) values of 1 indicates and additive drug interaction, whereas a CI of <1 is synergistic and a CI of >1 is antagonistic. |
| 别名 | LY2835219, CDK4/6 dual inhibitor |
| 分子量 | 506.59 |
| 分子式 | C27H32F2N8 |
| CAS No. | 1231929-97-7 |
| Smiles | C(C)(C)N1C=2C(=C(F)C=C(C2)C3=NC(NC4=CC=C(CN5CCN(CC)CC5)C=N4)=NC=C3F)N=C1C |
| 密度 | 1.32 g/cm3 (Predicted) |
| 颜色 | Yellow |
| 物理性状 | Solid |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||
| 溶解度信息 | DMSO: < 1 mg/mL (insoluble or slightly soluble), Sonication is recommended. Ethanol: 1.69 mg/mL (3.34 mM), Sonication is recommended. | ||||||||||
| 体内实验配方 | 10% DMSO+90% Saline: 0.1 mg/mL (0.2 mM), Solution. 请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。 | ||||||||||
溶液配制表 | |||||||||||
Ethanol
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Crystal structure of the human HIPK3 kinase domain bound to abemaciclib
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