NVP-ADW742 (Synonyms:ADW742; GSK 552602A; ADW)
目录号 : KM2436 CAS No. : 475488-23-4 纯度 : 98%

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)。

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2mg
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5mg
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10mg
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50mg
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100mg
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500mg 询价 In-stock

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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.

体外研究

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).

Cell Viability Assay

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

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

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.

Animal Model: 6- to 8-week-old male SCID/NOD mice with diffuse skeletal lesions of luciferase-expressing MM cells
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.
分子式
C28H31N5O
分子量
453.58
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。

  • 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。

  • 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。

科研文献
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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