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AZD1480

AZD1480是一种新型，ATP竞争性的JAK2抑制剂，IC50为0.26 nM，选择性作用于JAK3和Tyk2，对JAK1的作用较弱。

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生物活性

AZD1480 is a novel small-molecule JAK inhibitor. It is able to block cell proliferation and induce apoptosis of myeloma cell lines. It can effectively inhibit tumor angiogenesis and metastasis mediated by STAT3 in stromal cells as well as tumor cells. AZD1480 has broad efficacy on a wider variety of myeloma cells, such as RPMI 8226, OPM-2, NCI-H929, Kms.18, MM1.S and IM-9, as well as primary myeloma cells. AZD1480 induces cell death of Kms.11 cells grown in the presence of HS-5 bone marrow (BM)-derived stromal cells and inhibits tumor growth in a Kms.11 xenograft mouse model, accompanied with inhibition of phospho-FGFR3, phospho-JAK2, phospho-STAT3 and Cyclin D2 levels. AZD1480 also demonstrates important Jak2 selectivity over Jak3, in particular at high ATP concentrations and marginal selectivity over Jak1 at Km ATP.
体外研究
体内研究

30% PEG400+0.5% Tween80+5% Propylene glycol
激酶实验
细胞实验

1 μM
动物实验

每天一次，剂量为50 mg/kg；或者每天两次，剂量为30 mg/kg 口服饲喂
不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数

例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

参考文献

[1] E Derenzini, et al. Blood Cancer J, 2011, 1(12), e46.

分子式 C14H14ClFN8	分子量 348.77	CAS号 935666-88-9	储存方式 ﹣20 ℃冷藏长期储存。冰袋运输
溶剂（常温）	DMSO 70 mg/mL	Water <1 mg/mL	Ethanol <1 mg/mL

体内溶解度

NCT Number	Conditions	Interventions	Sponsor/Collaborators	Phases	Start Date	Last Updated
NCT01219543	Solid Tumour\|Advanced Solid Malignancies\|Child-Pugh A to B7 Advanced Hepatocellular Carcinoma\|EGFR and/or ROS Mutant NSCLC\|Lung Metastasis Carcinoma\|Gastric Cancer	Drug: AZD1480 Daily\|Drug: AZD1480 BID	AstraZeneca	Phase 1	2010-11-01	2013-01-07
NCT01112397	Solid Malignancies	Drug: AZD1480	AstraZeneca	Phase 1	2010-04-01	2013-07-19
NCT00910728	Primary Myelofibrosis (PMF)\|Post-Polycythaemia Vera\|Essential Thrombocythaemia Myelofibrosis	Drug: AZD1480	AstraZeneca\|University of Texas\|New York City Hoffman Center\|Gustave Roussy, Cancer Campus, Grand Paris	Phase 1	2009-05-01	2014-09-11

注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。