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, selectiveIGF-1Rtyrosine kinaseinhibitor with anIC50of 0.17 μM. NVP-ADW742 inhibitsinsulin receptor (InsR)with anIC50of 2.8 μM. NVP-ADW742 induces pleiotropic antiproliferative/proapoptoticbiologic 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 IC50values for other kinases (IC50>10 μM for HER2, PDGFR, VEGFR-2, or Bcr-Abl p210; and IC50>5 μM for c-Kit)[1].
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. |
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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].
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. |
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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 |
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溶解性数据 | In Vitro: DMSO : 19.23 mg/mL(42.40 mM;Need ultrasonic) 配制储备液 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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 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。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin 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 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 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本网站选购。
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