WHI-P180

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Chemical Structure| 211555-08-7 同义名 : Janex 3
CAS号 : 211555-08-7
货号 : A162125
分子式 : C16H15N3O3
纯度 : 98%
分子量 : 297.309
MDL号 : MFCD02683970
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(84.09 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 The RET receptor tyrosine kinase is crucial for normal development but also contributes to pathologies that reflect both the loss and the gain of RET function[3]. WHI-P180 is a multi-kinase inhibitor which inhibits RET, KDR and epidermal growth factor receptor (EGFR) with IC50s of 5 nM, 66 nM and 4 μM, respectively[4]. WHI-P180 is also an active inhibitor of IgE-mediated mast cell responses. The elimination half-life of WHI-P180 in CD-1 mice (BALB/c mice) following i.v., i.p., or p.o. administration is less than 10 min. Systemic clearance of WHI-P180 is 6742 mL/h/kg in CD-I mice and 8188 mL/h/kg in BALB/c mice. Notably, WHI-P180, when administered in two consecutive nontoxic i.p. bolus doses of 25 mg/kg, inhibits IgE/antigen-induced vascular hyperpermeability in a well-characterized murine model of passive cutaneous anaphylaxis[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.36mL

0.67mL

0.34mL

16.82mL

3.36mL

1.68mL

33.64mL

6.73mL

3.36mL
参考文献

[1]An R, Hagiya Y, et al. Cellular phototoxicity evoked through the inhibition of human ABC transporter ABCG2 by cyclin-dependent kinase inhibitors in vitro. Pharm Res. 2009 Feb;26(2):449-58.

[2]Chen CL, Malaviya R, et al. Pharmacokinetics and biologic activity of the novel mast cell inhibitor, 4-(3-hydroxyphenyl)-amino-6,7-dimethoxyquinazoline in mice. Pharm Res. 1999 Jan;16(1):117-22.

[3]Mulligan LM. RET revisited: expanding the oncogenic portfolio. Nat Rev Cancer. 2014 Mar;14(3):173-86. doi: 10.1038/nrc3680. PMID: 24561444.

[4]Ghosh S, Jennissen JD, Liu XP, Uckun FM. 4-[3-Bromo-4-hydroxyphenyl)amino]-6,7-dimethoxyquinazolin-1-ium chloride methanol solvate and 4-[(3-hydroxyphenyl)amino]-6,7-dimethoxy-1-quinazolinium chloride. Acta Crystallogr C. 2001 Jan;57(Pt 1):76-8. doi: 10.1107/s0108270100013561. PMID: 11173405.

[5]Chen CL, Malaviya R, Navara C, Chen H, Bechard B, Mitcheltree G, Liu XP, Uckun FM. Pharmacokinetics and biologic activity of the novel mast cell inhibitor, 4-(3-hydroxyphenyl)-amino-6,7-dimethoxyquinazoline in mice. Pharm Res. 1999 Jan;16(1):117-22. doi: 10.1023/a:1018835232027. PMID: 9950289.