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Acalabrutinib (Synonyms: ACP-196) 纯度: 99.94%
Acalabrutinib (ACP-196) 是一种具有口服活性,不可逆的,高度选择性的第二代 BTK 抑制剂。Acalabrutinib 与 BTK 的 ATP 结合口袋中的 Cys481 共价结合。Acalabrutinib 在慢性淋巴细胞性白血病 (CLL) 小鼠模型中显示出强大的靶向作用和功效。
Acalabrutinib Chemical Structure
CAS No. : 1420477-60-6
规格 | 价格 | 是否有货 | 数量 |
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Free Sample (0.1-0.5 mg) | Apply now | ||
10 mM * 1 mL in DMSO | ¥660 | In-stock | |
2 mg | ¥400 | In-stock | |
5 mg | ¥600 | In-stock | |
10 mg | ¥1000 | In-stock | |
50 mg | ¥3200 | In-stock | |
100 mg | ¥5150 | In-stock | |
200 mg | ¥8240 | In-stock | |
500 mg | 询价 | ||
1 g | 询价 |
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Acalabrutinib 相关产品
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生物活性 |
Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor. Acalabrutinib binds covalently to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib demonstrates potent on-target effects and efficacy in mouse models of chronic lymphocytic leukemia (CLL)[1][2]. |
IC50 & Target |
IC50: 3 nM (BTK in CD69 B cell)[2] |
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体外研究 (In Vitro) |
Acalabrutinib (ACP-196) inhibits tyrosine phosphorylation of downstream targets of ERK, IKB, and AKT, in the in vitro signaling assay on primary human CLL cells. In the human CLL NSG xenograft model, Acalabrutinib demonstrates on-target effects including decreased phosphorylation of PLCγ2, ERK and significant inhibition of CLL cell proliferation[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (In Vivo) |
Acalabrutinib (100 mg twice per day) assessed for thrombus formation at injured arterioles of the mice, exhibits more selective for inhibiting BTK and has virtually no inhibition of platelet activity[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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Clinical Trial |
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分子量 |
465.51 |
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Formula |
C26H23N7O2 |
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CAS 号 |
1420477-60-6 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : 250 mg/mL (537.05 mM; Need ultrasonic) 配制储备液
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
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参考文献 |
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