产品说明书

PQ401

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Chemical Structure| 196868-63-0 同义名 : -
CAS号 : 196868-63-0
货号 : A165138
分子式 : C18H16ClN3O2
纯度 : 99%+
分子量 : 341.791
MDL号 : MFCD00160558
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 15 mg/mL(43.89 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 2% DMSO+2% Tween80+40% PEG300+water 10 mg/mL clear

PO 0.5% CMC-Na 63 mg/mL suspension

生物活性
靶点

  • IGF-1R

    IGF-1R, IC50:<1 μM
描述 The insulin-like growth factor receptor (IGF-IR) is a transmembrane protein, signaling via the tyrosine kinase domain of which is important for normal cell growth and differentiation. In addition, the IGF-IR stimulates mitogenesis and suppresses apoptosis of cancer cells. PQ401 is a potent inhibitor of IGF-IR signaling which inhibits autophosphorylation of IGF-IR with an IC50 less than 1 μM. PQ401 significantly reduced the proliferation of MCF-7 cells grown in serum with an IC50 of 8 μM. PQ401 also inhibited the growth of MCNeuA cells with an IC50 of 15 μM. PQ401 (15 μM; 24 h) induced caspase-mediated apoptosis. In vivo, PQ401 (50 or 100 mg/kg; i.p.; three times per week) resulted in a significant dose-dependent reduction in tumor growth in female mice model bearing MCNeuA tumor cells[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.93mL

0.59mL

0.29mL

14.63mL

2.93mL

1.46mL

29.26mL

5.85mL

2.93mL
参考文献

[1]Troib A, Landau D, et al. 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.

[2]Gable KL, Maddux BA, et al. 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.

[3]Gable KL, et al. 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.