NVP-ADW742 (Synonyms: ADW742; GSK 552602A; ADW)
目录号: PL01359 纯度: ≥99%
CAS No. :475488-23-4
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中文名称
NVP-ADW742
中文别名
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;5-[3-(苯基甲氧基)苯基]-7-[反式-3-(1-吡咯烷甲基)环丁基]-[反式-3-(1-吡咯烷甲基)环丁基]-7H-吡咯并[2,3-d]嘧啶-4-胺;NVP-ADW742 抑制剂
英文名称
NVP-ADW742
英文别名
5-(3-Benzyloxyphenyl)-7-[trans-3-[(pyrrolidin-1-yl)methyl]cyclobutyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine;NVP-ADW742;5-(3-(Benzyloxy)phenyl)-7-((1r,3r)-3-(pyrrolidin-1-ylmethyl)-cyclobutyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine;5-(3-phenylmethoxyphenyl)-7-[3-(pyrrolidin-1-ylmethyl)cyclobutyl]pyrrolo[2,3-d]pyrimidin-4-amine;NVP ADW 742;ADW;ADW742;ADW742,NVP-ADW742;GSK 552602A;Kinome_2540;5-[3-(Phenylmethoxy)phenyl]-7-[trans-3-(1-pyrrolidinylmethyl)cyclobutyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine
Cas No.
475488-23-4
分子式
C28H31N5O
分子量
453.58
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
NVP-ADW742 (ADW742) 是一种具有口服活性,选择性的 IGF-1R 酪氨酸激酶抑制剂,IC50 为 0.17 μM。NVP-ADW742 抑制胰岛素受体 (InsR),IC50 为 2.8 μM。NVP-ADW742 在肿瘤细胞中诱导多效性抗增殖/促凋亡 (apoptosis)。
生物活性
NVP-ADW742 (ADW742) is an orally active, selective IGF-1R tyrosine kinase inhibitor with an IC 50 of 0.17 μM. NVP-ADW742 inhibits insulin receptor (InsR) with an IC 50 of 2.8 μM. NVP-ADW742 induces pleiotropic antiproliferative/proapoptotic biologic sequelae in tumor cells.
性状
Solid
IC50 & Target[1][2]
IC50: 0.17 μM (IGF-1R) and 2.8 μM (InsR)
体外研究(In Vitro)
NVP-ADW742 (ADW742; 0.1-10 μM; 72 hours) dose-dependently inhibits serum-induced cell growth in all cell lines.
NVP-ADW742 (0.1-9 μM; 20 min) blocks IGF-1-induced phosphorylation of IGF-1R and its known downstream target Akt at submicromolar concentrations.
NVP-ADW742 has much higher IC50 values for other kinases (IC50>10 μM for HER2, PDGFR, VEGFR-2, or Bcr-Abl p210; and IC50>5 μM for c-Kit).
has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
NVP-ADW742 (ADW742; 10 mg/kg for IP or 50 mg/kg for orally; twice daily for 19 days) significantly suppresses tumor growth and prolongs the survival of mice.
has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Mitsiades CS, et 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 GS, et al. The insulin-like growth factor-I (IGF-I) receptor kinase inhibitor NVP-ADW742, in combination with STI571, delineates a spectrum of dependence of small cell lung cancer on IGF-I and stem cell factor signaling. Mol Cancer Ther.
溶解度数据
In Vitro: DMSO : 19.23 mg/mL (42.40 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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