AZD1480
(Synonyms: 5-氯-N2-[(1S)-1-(5-氟-2-嘧啶基)乙基]-N4-(5-甲基-1H-吡唑-3-基)-2,4-嘧啶二胺,AZD 1480) 目录号 : GC12504
A potent JAK2 inhibitor
Cas No.:935666-88-9
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment: [1] | |
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Cell lines |
SKOV3 cells |
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Preparation method |
The solubility of this compound in DMSO is >93.8mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
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Reaction Conditions |
10 μM, 24 hours |
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Applications |
In the AZD1480 combined with cisplatin treatment groups, cisplatin could inhibit the proliferation of SKOV3 cells with dose dependent (P0.05) butwas statistically significant difference 5 μmol/L and 10 μmol/L AZD148 groups compared with the control group (P |
| Animal experiment: [2] | |
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Animal models |
SCID/Beige mice injected with TC32 or Rh18 cells |
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Dosage form |
Oral administration, 30 mg/kg, twice a day for 21 days |
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Applications |
The tumor growth in AZD1480-treated group was significantly depressed compared to control in each cell line. Tumors from mice treated with AZD1480 had decreased levels of tyrosine phosphorylated STAT3 as well as of STAT3 downstream targets (CyclinD1,-3, Bcl-2 and Survivin) compared to the levels in tumors from mice receiving vehicle. This shows that AZD1480 treatment induces the inhibition of STAT3 activity and its target gene expression in vivo. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Xin Y L Y, Yang Y, Han P. AZD1480 can inhibit the biological behavior of ovarian cancer SKOV3 cells in vitro. Asian Pacific Journal of Cancer Prevention, 2013, 14(8): 4823-4827. [2] Yan S, Li Z, Thiele C J. Inhibition of STAT3 with orally active JAK inhibitor, AZD1480, decreases tumor growth in Neuroblastoma and Pediatric Sarcomas In vitro and In vivo. Oncotarget, 2013, 4(3): 433. |
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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.
Reference
[1].A Scuto, P Krejci, L Popplewell, J Wu, Y Wang, M Kujawski, C Kowolik, H Xin, L Chen, Y Wang, L Kretzner, H Yu, W R Wilcox, Y Yen, S Forman and R Jove. The novel JAK inhibitor AZD1480 blocks STAT3 and FGFR3 signaling, resulting in suppression of human myeloma cell growth and survival. Leukemia. 2011 March ; 25(3): 538–550
[2].Michael Hedvat, Dennis Huszar, Andreas Herrmann, Joseph M. Gozgit, Anne Schroeder, Adam Sheehy, Ralf Buettner, David Proia, Claudia M. Kowolik, Hong Xin, Brian Armstrong, Geraldine Bebernitz, Shaobu Weng, Lin Wang, Minwei Ye, Kristen McEachern, Huawei Chen, Deborah Morosini, Kirsten Bell, Marat Alimzhanov, Stephanos Ioannidis, Patricia McCoon, Zhu A. Cao, Hua Yu, Richard Jove, Michael Zinda. The JAK2 Inhibitor AZD1480 Potently Blocks Stat3 Signaling and Oncogenesis in Solid Tumors. Cancer Cell. 2009; 16 (6): 487–497
[3].Hong Xin, Andreas Herrmann, Karen Reckamp, Wang Zhang, Sumanta Pal, Michael Hedvat, Chunyan Zhang, Wei Liang, Anna Scuto, Shaobu Weng, Deborah Morosini, Zhu A. Cao, Michael Zinda, Robert Figlin, Dennis Huszar, Richard Jove, Hua Yu. Antiangiogenic and Antimetastatic Activity of JAK Inhibitor AZD1480. Cancer Research. 2011;71: 6601-6610
| Cas No. | 935666-88-9 | SDF | |
| 别名 | 5-氯-N2-[(1S)-1-(5-氟-2-嘧啶基)乙基]-N4-(5-甲基-1H-吡唑-3-基)-2,4-嘧啶二胺,AZD 1480 | ||
| 化学名 | 5-chloro-2-N-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-4-N-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine | ||
| Canonical SMILES | CC1=CC(=NN1)NC2=NC(=NC=C2Cl)NC(C)C3=NC=C(C=N3)F | ||
| 分子式 | C14H14ClFN8 | 分子量 | 348.77 |
| 溶解度 | ≥ 93.8 mg/mL in DMSO, ≥ 4.57 mg/mL in EtOH with ultrasonic and warming | 储存条件 | Store at -20°C |
| General tips | 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。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8672 mL | 14.3361 mL | 28.6722 mL |
| 5 mM | 0.5734 mL | 2.8672 mL | 5.7344 mL |
| 10 mM | 0.2867 mL | 1.4336 mL | 2.8672 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。