AZD-1480
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Cat.No：IA1630 Solarbio
CAS：935666-88-9
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Solid
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> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > JAK/STAT > AZD-1480
Product Information
| CAS | 935666-88-9 |
| Name | AZD-1480 |
| Molecular Formula | C14H14ClFN8 |
| Molecular Weight | 348.77 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| Delivery Time | 1-2 Days |
| MDL | MFCD16038904 |
| SMILES | ClC1=C(N=C(N=C1)N[C@@H](C)C2=NC=C(C=N2)F)NC3=NNC(C)=C3 |
| InChIKey | PDOQBOJDRPLBQU-QMMMGPOBSA-N |
| InChI | InChI=1S/C14H14ClFN8/c1-7-3-11(24-23-7)21-13-10(15)6-19-14(22-13)20-8(2)12-17-4-9(16)5-18-12/h3-6,8H,1-2H3,(H3,19,20,21,22,23,24)/t8-/m0/s1 |
| PubChem CID | 16659841 |
| Target Point | JAK |
| Passage | JAK/STAT Signaling |
| Background | AZD-1480 is a novel ATP-competitive inhibitor of JAK2 |
| Biological Activity | AZD-1480 是一种新颖的 JAK2 的ATP竞争性抑制剂，IC50 值为 < 0.4 nM[1-6]。 |
| IC50 | JAK1:1.3nM;JAK2:0.4nM [1-6] |
| In Vitro | AZD1480是一种有效的JAK2抑制剂，可抑制人多发性骨髓瘤细胞的生长，存活，以及FGFR3和STAT3信号传导以及下游靶标，包括Cyclin D2。在低微摩尔浓度下，AZD1480阻断细胞增殖并诱导骨髓瘤细胞系的凋亡[2]。AZD1480有效阻断人和小鼠胶质瘤细胞中组成型和刺激诱导的JAK1，JAK2和STAT-3磷酸化，并导致细胞增殖减少和细胞凋亡诱导[3]。 AZD1480是一种有效的，竞争性的JAK1/2激酶小分子抑制剂，能够以STAT3依赖性方式抑制STAT3磷酸化和肿瘤生长。 AZD1480通过影响肿瘤微环境来抑制肿瘤血管生成和转移[4]。AZD1480(5μM)通过抑制Aurora激酶诱导G2/M阻滞和细胞死亡[1]。 |
| In Vivo | 在体内，AZD1480通过抑制STAT-3活性抑制皮下肿瘤的生长并增加携带颅内胶质母细胞瘤(GBM)肿瘤的小鼠的存活率，表明AZD1480对JAK/STAT-3途径的药理学抑制应考虑用于研究。治疗GBM肿瘤患者[3]。在小鼠同系实验和自发转移模型中，AZD1480阻断骨髓细胞的肺浸润和肺转移的形成。此外，AZD1480可减少人类异种移植肿瘤模型中的血管生成和转移[4]。 AZD1480抑制具有持久Stat3活性的人类实体瘤异种移植物的生长[5]。AZD1480抑制人类实体瘤和多发性骨髓瘤的异种移植模型中的STAT3磷酸化[1]。 |
| Cell Experiment | 将Renca或786-O细胞悬浮于含有5％FBS的DMEM培养基中，并接种于96孔板(每孔5×103)中以使其粘附，然后用DMSO或AZD1480处理48小时。通过MTS测定确定细胞活力。用Mikrotek Laborsysteme测量490nm处的吸光度。从携带肿瘤的小鼠中富集小鼠内皮细胞和脾CD11b +/c-髓样细胞，并在5％FBS RPMI-1640培养基中培养。 HUVEC在完全培养基中的胶原蛋白1包被的平板上培养。用DMSO和AZD1480以不同剂量处理所有细胞24小时。通过手动计数细胞数确定细胞活力。所有实验重复3次。 |
| Animal Experiment | 对于皮下(sc)肿瘤模型，将悬浮在100μLPBS中的2.5×106 Renca或786-O细胞分别注射到BALB/c或裸鼠的胁腹中。当平均肿瘤体积达到约100-150mm 3时，如所示，AZD1480或载体通过口服管饲法以50mg/kg的剂量每天一次或每天两次以30mg/kg给药。每隔一天用卡尺测量肿瘤大小。对于实验性肺转移模型，将悬浮在500μLPBS中的0.1×106 Renca或1×106 786-O细胞分别通过尾静脉注射到BALB/c或裸鼠。三天后，分别用AZD1480(50mg/kg/d)或载体口服小鼠Renca肿瘤21天和786-O肿瘤60天。对于Calu-6模型，将基质胶中的3×106个肿瘤细胞皮下植入裸鼠的侧腹，随机分入载体(每日两次，BID)和药物治疗(AZD1480，30mg/kg BID)组，并口服给药每天19天。对于自发性肺转移模型，通过轻柔地穿透皮肤，将悬浮在100μLPBS中的2×105个4T1细胞注射到雌性BALB/c小鼠的乳腺中。 AZD1480(50mg/kg/d)或载体口服给药21天。 |
| Kinase Experiment | 使用重组Jak1，Jak2或Jak3在50mM HEPES pH 7.3，1mM DTT，0.01％Tween-20，50mM/mL BSA和10mM MgCl 2的缓冲条件下进行AZD1480的抑制研究。 Jak3酶在昆虫细胞中表达为N-末端GST融合物，并通过谷胱甘肽亲和力和尺寸排阻色谱法纯化。使用1.5μM肽底物(Jak1：FITC-C6-KKHTDDGYMPMSPGVA-NH2，Jak2和Jak3：)在AZD1480(10点剂量反应，一式三份，半对数稀释步骤中从8.3μM至0.3nM)存在下测定酶。 FAM-SRCtide)并在它们各自的ATP Km(Jak1：55μM，Jak2：15μM，Jak3：3μM)下筛选并且接近5mM的生理ATP浓度。通过Caliper LC3000系统分离和定量磷酸化和未磷酸化的肽以计算抑制百分比。 |
| Data Literature Source | [1]. Derenzini E，et al. The JAK inhibitor AZD1480 regulates proliferation and immunity in Hodgkin lymphoma. Blood Cancer J. 2011 Dec;1(12):e46. [2]. Scuto A，et al. The novel JAK inhibitor AZD1480 blocks STAT3 and FGFR3 signaling，resulting in suppression of human myeloma cell growth and survival. Leukemia. 2011 Mar;25(3):538-50. [3]. McFarland BC，et al. Therapeutic potential of AZD1480 for the treatment of human glioblastoma. Mol Cancer Ther. 2011 Dec;10(12):2384-93. [4]. Xin H，et al. Antiangiogenic and antimetastatic activity of JAK inhibitor AZD1480. Cancer Res. 2011 Nov 1;71(21):6601-10. [5]. Hedvat M，et al. The JAK2 inhibitor AZD1480 potently blocks Stat3 signaling and oncogenesis in solid tumors. Cancer Cell. 2009 Dec 8;16(6):487-9 [6]. Ni J，et al. Tyrosine receptor kinase B is a drug target in astrocytomas. Neuro Oncol. 2017 Jan;19(1):22-30. |
| Unit | Bottle |
| Specification | 5mg 10mg |
是一种新颖的 JAK2 的ATP竞争性抑制剂
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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2. For your safety and health, please wear laboratory clothes, disposable gloves and masks.
3. The experimental results may be affected by many factors, after-sale service is limited to the product itself and does not involve other compensation.
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