NVP-ADW742
(Synonyms: 5-(3-苄氧基苯基)-7-[反式-3-[(吡咯烷-1-基)甲基]环丁基]-7H-吡咯并[2,3-D]嘧啶-4-胺,ADW742; GSK 552602A; ADW) 目录号 : GC14310
An IGF-1R inhibitor
Cas No.:475488-23-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
NVP-ADW742 is a novel inhibitor of IFG-1receptor (IGF-1R) kinase with the IC50 value of 0.17μM [1].
NVP-ADW742 has shown above 16-fold effective function against IGF-1R than insulin receptor (InsR). Furthermore, NVP-ADW742 has also been reported to inhibit other kinases , with the IC50 values of ＞10μM for HER2, PDGFR, VEGFR-2, or Bcr-Abl p210, and the IC50 values ＞5μM for c-Kit [1]. Besides, NVP-ADW742 combined with etoposide and carboplatin has been reported to inhibit cell growth and induce cytotoxicity by MTT assay using the small cell lung cancer (SCLC), including H526, H146, WBA and H209 cell lines. In addition, NVP-ADW742 has been revealed to completely inhibit the expression of VEGF mRNA which induced by IGF-I in H526 cells [2].
References:
[1] Mitsiades CS1, Mitsiades NS, McMullan CJ, Poulaki V, Shringarpure R, Akiyama M, Hideshima T, Chauhan D, Joseph M, Libermann TA, García-Echeverría C, Pearson MA, Hofmann F, Anderson KC, Kung AL. Inhibition of the insulin-like growth factor receptor-1 tyrosine kinase activity as a therapeutic strategy for multiple myeloma, other hematologic malignancies, and solid tumors . Cancer Cell. 2004 Mar; 5(3):221-30.
[2]Warshamana-Greene GS1, Litz J, Buchdunger E, García-Echeverría C, Hofmann F, Krystal GW. The insulin-like growth factor-I receptor kinase inhibitor, NVP-ADW742, sensitizes small cell lung cancer cell lines to the effects of chemotherapy. Clin Cancer Res. 2005 Feb 15;11(4):1563-71.
| Cas No. | 475488-23-4 | SDF | |
| 别名 | 5-(3-苄氧基苯基)-7-[反式-3-[(吡咯烷-1-基)甲基]环丁基]-7H-吡咯并[2,3-D]嘧啶-4-胺,ADW742; GSK 552602A; ADW | ||
| 化学名 | 5-(3-phenylmethoxyphenyl)-7-[3-(pyrrolidin-1-ylmethyl)cyclobutyl]pyrrolo[2,3-d]pyrimidin-4-amine | ||
| Canonical SMILES | C1CCN(C1)CC2CC(C2)N3C=C(C4=C3N=CN=C4N)C5=CC(=CC=C5)OCC6=CC=CC=C6 | ||
| 分子式 | C28H31N5O | 分子量 | 453.58 |
| 溶解度 | DMF: 30 mg/mL,DMSO: 30 mg/mL,Ethanol: 30 mg/mL,Ethanol:PBS (pH 7.2) (1:10): 0.09 mg/mL | 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 | 2.2047 mL | 11.0234 mL | 22.0468 mL |
| 5 mM | 0.4409 mL | 2.2047 mL | 4.4094 mL |
| 10 mM | 0.2205 mL | 1.1023 mL | 2.2047 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。