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Seralutinib

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Chemical Structure| 1619931-27-9 同义名 : GB002;PK10571
CAS号 : 1619931-27-9
货号 : A1376658
分子式 : C27H27N5O3
纯度 : 99%+
分子量 : 469.535
MDL号 : MFCD28502207
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 190 mg/mL(404.66 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：
生物活性
描述 Platelet-derived growth factor (PDGF) was discovered as a serum-derived component necessary for the growth of smooth muscle cells, fibroblasts, and glial cells. Although PDGF signaling is most closely associated with mesenchymal cells, PDGFs and PDGF receptors are widely expressed in the mammalian central nervous system[2]. Today the PDGF family of growth factors consists of five different disulphide-linked dimers built up of four different polypeptide chains encoded by four different genes. These isoforms, PDGF-AA, PDGF-AB, PDGF-BB, PDGF-CC and PDGF-DD, act via two receptor tyrosine kinases, PDGF receptors alpha and beta[3]. PDGFRα expression decreases with adipocyte lineage, while PDGFRβ inhibits white adipocyte differentiation. In addition, PDGFRβ induces proliferation, migration, and angiogenesis and up-regulates the expression of paracrine factors in adipose-derived stem cells(ASCs)[4].Overactivity of PDGF receptor signaling, by overexpression or mutational events, may drive tumor cell growth. In addition, pericytes of the vasculature and fibroblasts and myofibroblasts of the stroma of solid tumors express PDGF receptors, and PDGF stimulation of such cells promotes tumorigenesis[5]. Seralutinib(GB002) is an inhibitor of inhaled PDGFRα and PDGFRβ. It is used in the study for pulmonary arterial hypertension.GB002 dose-and time-dependently induces lung BMPR2 protein expression.GB002-mediated inhibition of lung PDGFRα/β phosphorylation in healthy Sprague Dawley rats immediately post inhalation[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.13mL

0.43mL

0.21mL

10.65mL

2.13mL

1.06mL

21.30mL

4.26mL

2.13mL
参考文献

[1]Abstract 11102: Gb002, A Novel Inhaled Pdgfr Kinase Inhibitor, Demonstrates Efficacy in the Su5416 Hypoxia Rat Model of Pulmonary Arterial Hypertension (pah)

[2] Robert Roskoski Jr. The role of small molecule platelet-derived growth factor receptor (PDGFR) inhibitors in the treatment of neoplastic disorders. Pharmacol Res. 2018 Mar;129:65-83.

[3]Linda Fredriksson, Hong Li, Ulf Eriksson. The PDGF family: four gene products form five dimeric isoforms. Cytokine Growth Factor Rev. 2004 Aug;15(4):197-204.

[4] Won-Serk Kim,et al. The pivotal role of PDGF and its receptor isoforms in adipose-derived stem cells. Histol Histopathol. 2015 Jul;30(7):793-9.

[5]Carl-Henrik Heldin. Targeting the PDGF signaling pathway in tumor treatment. Cell Commun Signal. 2013 Dec 20;11:97.

[6] 1. Anna Galkin, et al. Pharmacologic Characterization of GB002, a Novel Inhaled PDGFR Kinase Inhibitor in Development for Pulmonary Arterial Hypertension (PAH).