AC710
(Synonyms: N-[4-[[[[5-(叔丁基)-3-异恶唑基]氨基]羰基]氨基]苯基]-5-[(1-乙基-2,2,6,6-四甲基-4-哌啶基)氧基]-2-吡啶甲酰胺) 目录号 : GC18167
A PDGFR family kinase inhibitor
Cas No.:1351522-04-7
Sample solution is provided at 25 µL, 10mM.
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AC710 is a potent, orally active, and selective platelet-derived growth factor receptor-family kinase inhibitor with potential anticancer activity. Its IC50 values are 1.2, 2, 7.7 and 10.5 nM for KIT, FLT3, PDGFRβ and CSF1R respectively; Kd = 1.3 nM for PDGFRα.. AC710 causes tumor regression of leukemia cell xenografts in mice. AC710 also reduces joint swelling and inflammation in a mouse model of collagen-induced arthritis. AC710 is now a preclinical development candidate.
REFERENCES:
Liu *†, Brian T. Campbell †, Mark W. Holladay †, Julia M. Ford Pulido ‡, Helen Hua ‡, Dana Gitnick , Michael F. Gardner , Joyce James , Mike A. Breider , Daniel Brigham ‡, Barbara Belli ‡, Robert C. Armstrong ‡, and Daniel K. Treiber. Discovery of AC710, a Globally Selective Inhibitor of Platelet-Derived Growth Factor Receptor-Family Kinases. ACS Med. Chem. Lett., 2012, 3 (12), pp 997–1002
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Animal experiment: |
Mice: The antitumor efficacy of AC710 is assessed in a subcutaneous flank-tumor xenograft model in athymic nude mice using the MV4-11cell line. AC710 is dosed at 0.3, 3, and 30 mg/kg for 2 weeks. Tumor growth and body weight is monitored[1]. |
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References: [1]. Liu G, et al. Discovery of AC710, a Globally Selective Inhibitor of Platelet-Derived Growth Factor Receptor-Family Kinases. ACS Med Chem Lett. 2012 Sep 24;3(12):997-1002. |
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| Cas No. | 1351522-04-7 | SDF | |
| 别名 | N-[4-[[[[5-(叔丁基)-3-异恶唑基]氨基]羰基]氨基]苯基]-5-[(1-乙基-2,2,6,6-四甲基-4-哌啶基)氧基]-2-吡啶甲酰胺 | ||
| 化学名 | N-(4-(3-(5-(tert-butyl)isoxazol-3-yl)ureido)phenyl)-5-((1-ethyl-2,2,6,6-tetramethylpiperidin-4-yl)oxy)picolinamide | ||
| Canonical SMILES | O=C(NC1=CC=C(NC(NC2=NOC(C(C)(C)C)=C2)=O)C=C1)C3=NC=C(OC4CC(C)(C)N(CC)C(C)(C)C4)C=C3 | ||
| 分子式 | C31H42N6O4 | 分子量 | 562.7 |
| 溶解度 | DMF:10 mg/ml; DMSO:14 mg/mL (24.88 mM; Need 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 | 1.7771 mL | 8.8857 mL | 17.7715 mL |
| 5 mM | 0.3554 mL | 1.7771 mL | 3.5543 mL |
| 10 mM | 0.1777 mL | 0.8886 mL | 1.7771 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。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet