NVP-ADW742(Synonyms: ADW742; GSK 552602A; ADW)

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NVP-ADW742 (Synonyms: ADW742; GSK 552602A; ADW) 纯度: 99.30%

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)。

NVP-ADW742(Synonyms: ADW742; GSK 552602A; ADW)

NVP-ADW742 Chemical Structure

CAS No. : 475488-23-4

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1197 In-stock
2 mg ￥800 In-stock
5 mg ￥1200 In-stock
10 mg ￥2000 In-stock
50 mg ￥6700 In-stock
100 mg ￥12000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

NVP-ADW742 相关产品

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生物活性

NVP-ADW742 (ADW742) is an orally active, selective IGF-1R tyrosine kinase inhibitor with an IC50 of 0.17 μM. NVP-ADW742 inhibits insulin receptor (InsR) with an IC50 of 2.8 μM. NVP-ADW742 induces pleiotropic antiproliferative/proapoptotic biologic sequelae in tumor cells[1][2].

IC50 & Target

IC50: 0.17 μM (IGF-1R) and 2.8 μM (InsR)[1]
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[1].
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[1].
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)[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: A panel of cell lines from multiple myeloma (MM), other hematologic malignancies and solid tumors
Concentration: 0.1, 0.5, 1, 2, 5, 10 µM
Incubation Time: 72 hours
Result: Dose-dependently inhibited serum-induced cell growth in all cell lines.

Western Blot Analysis[1]

Cell Line: NWT-21 cells
Concentration: 0.1, 0.3, 1, 3, 9 µM
Incubation Time: 20 min
Result: Blocked IGF-1-induced phosphorylation of IGF-1R and its known downstream target Akt at submicromolar concentrations.

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[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 6- to 8-week-old male SCID/NOD mice with diffuse skeletal lesions of luciferase-expressing MM cells[1]
Dosage: 10 mg/kg (IP) or 50 mg/kg (orally)
Administration: IP or orally; twice daily for 19 days
Result: Significantly suppressed tumor growth and prolonged the survival of mice.

分子量

453.58

Formula

C28H31N5O
CAS 号

475488-23-4
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
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 19.23 mg/mL (42.40 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 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

*

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, 6 months; -20°C, 1 month。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 1.92 mg/mL (4.23 mM); Suspended solution; Need ultrasonic

    此方案可获得 1.92 mg/mL (4.23 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 19.2 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 1.92 mg/mL (4.23 mM); Suspended solution; Need ultrasonic

    此方案可获得 1.92 mg/mL (4.23 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 19.2 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 1.92 mg/mL (4.23 mM); Clear solution

    此方案可获得 ≥ 1.92 mg/mL (4.23 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 19.2 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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. 2004 May;3(5):527-35.

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