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PQ401

PQ401用途

PQ401是IGF1R阻断剂,能抑制IGF1R自磷酸化,IC50 < 1 uM。

PQ401名称

[ CAS 号 ]:
196868-63-0

[ 中文名 ]:
1-(5-氯-2-甲氧基苯基)-3-(2-甲基喹啉-4-基)脲

[ 英文名 ]:
PQ 401

[中文别名 ]:

[英文别名 ]:

IGF-1R Inhibitor II
UNII-2N3LV83S8J
TCMDC-125497
PQ 401
PQ401

PQ401生物活性

[ 描述 ]:

PQ401是IGF1R阻断剂,能抑制IGF1R自磷酸化,IC50 < 1 uM。

[ 相关类别 ]:

信号通路 >> 蛋白酪氨酸激酶 >> IGF-1R

研究领域 >> 癌症

[参考文献]

[1]. Gable KL, Maddux BA, Penaranda C, Diarylureas are small-molecule inhibitors of insulin-like growth factor I receptor signaling and breast cancer cell growth. Mol Cancer Ther. 2006 Apr;5(4):1079-86.

[2]. Troib A, Landau D, Youngren JF, The effects of type 1 IGF receptor inhibition in a mouse model of diabetic kidney disease. Growth Horm IGF Res. 2011 Oct;21(5):285-91.

[3]. Sanchez-Alavez M, Osborn O, Tabarean IV, Insulin-like growth factor 1-mediated hyperthermia involves anterior hypothalamic insulin receptors. J Biol Chem. 2011 Apr 29;286(17):14983-90.

[4]. Youssif C, et al. Myeloid p38α signaling promotes intestinal IGF-1 production and inflammation-associated tumorigenesis. EMBO Mol Med. 2018 Jul;10(7). pii: e8403.

[相关活性小分子]

PQ401物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
426.1±45.0 °C at 760 mmHg

[ 熔点 ]:
190 °C(dec.)

[ 分子式 ]:
C₁₈H₁₆ClN₃O₂

[ 分子量 ]:
341.792

[ 闪点 ]:
211.5±28.7 °C

[ 精确质量 ]:
341.093109

[ PSA ]:
63.25000

[ LogP ]:
5.35

[ 外观性状 ]:
white

[ 蒸汽压 ]:
0.0±1.0 mmHg at 25°C

[ 折射率 ]:
1.709

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
DMSO: >10mg/mL

PQ401MSDS

详细MSDS(安全技术说明书)

PQ401安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301

[ 警示性声明 ]:
P301 + P310

[ 个人防护装备 ]:
Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T: Toxic;

[ 风险声明 (欧洲) ]:
R25

[ 安全声明 (欧洲) ]:
S45

[ 危险品运输编码 ]:
UN 2811 6.1/PG 3

[ 海关编码 ]:
2933499090

PQ401海关

[ 海关编码 ]: 2933499090

[ 中文概述 ]:
2933499090. 其他含喹琳或异喹啉环系的化合物〔但未进一步稠合的〕. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933499090. other compounds containing in the structure a quinoline or isoquinoline ring-system (whether or not hydrogenated), not further fused. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

PQ401文献

Identification of Novel IGF1R Kinase Inhibitors by Molecular Modeling and High-Throughput Screening.

Acta Naturae 5(2) , 90-9, (2013)

The aim of this study was to identify small molecule compounds that inhibit the kinase activity of the IGF1 receptor and represent novel chemical scaffolds, which can be potentially exploited to devel...

IGFBP-2 directly stimulates osteoblast differentiation.

J. Bone Miner Res. 29(11) , 2427-38, (2014)

Insulin-like growth factor binding protein 2 (IGFBP-2) is important for acquisition of normal bone mass in mice; however, the mechanism by which IGFBP-2 functions is not defined. These studies investi...

Diarylureas are small-molecule inhibitors of insulin-like growth factor I receptor signaling and breast cancer cell growth.

Mol. Cancer Ther. 5 , 1079-1086, (2006)

In breast and certain other cancers, receptor tyrosine kinases, including the insulin-like growth factor I receptor (IGF-IR), play an important role in promoting the oncogenic process. The IGF-IR is t...

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