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Apilimod mesylate

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Chemical Structure| 870087-36-8 同义名 : 阿吡莫德甲磺酸盐 ;STA 5326 mesylate;LAM-002A;AIT-101 mesylate
CAS号 : 870087-36-8
货号 : A140672
分子式 : C25H34N6O8S2
纯度 : 99%+
分子量 : 610.703
MDL号 : MFCD28167749
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: 12 mg/mL(19.65 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

H2O: 100 mg/mL(163.75 mM)，配合低频超声助溶
动物实验配方：
生物活性
描述 Phosphatidylinositol-3-phosphate 5-kinase (PIKfyve) is a lipid kinase that synthesizes two phosphoinositides (PIs), regulating degradative and recycling endosomal trafficking, cytoskeletal rearrangement and autophagy. Apilimod Mesylate is a mesylate form of Apilimod. Apilimod is a 1,3,5-triazine derivative that binds to and inhibits PIKfyve kinase activity with an IC50 value of 14 nM. Treatment of apilimod (10 nM and 1 μM) for 120min decreased PI(3,5)P2 in HeLa cells at a dose-dependent manner. RAW264.7 cells treated with 10 nM Apilimod for 3h showed enlarged vacuoles due to the disruption of PIKfyve activity. In A549 cells, overexpression of wild-type PIKfyve resulted in the disappearance of vacuoles induced by 10 nM apilimod. Bone-marrow-derived dendritic cells from mutant mice demonstrated extensive vacuole formation with the treatment of 1 μM apilimod[3]. Apilimod showed selective antiproliferative activity in B-NHL cells with an IC50 value of 142 nM. After the treatment of 200 nM apilimod for 3 days, increased apoptosis was shown in SU-DHL-10 B-NHL cells. In a subcutaneous daudi burkitt lymphoma xenograft model, apilimod (50 - 150 mg/kg free base; p.o., once a day) displayed tumor growth inhibition at a dose-dependent manner. The growth inhibition was also observed in SU-DHL-6 DLBCL model treated with both apilimod (41 mg/kg free base, p.o., twice a day) and rituximab (7 mg/kg, i.p.)[4].
作用机制 Apilimod is a potent, highly selective PIKfyve inhibitor that binds to the PIKfyve domain (amino acids 1522 to 2098) to block the phosphotransferase activity of PIKfyve, thereby inhibiting IL-12/23p40[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.64mL

0.33mL

0.16mL

8.19mL

1.64mL

0.82mL

16.37mL

3.27mL

1.64mL
参考文献

[1]Gayle S, Landrette S, et al. Identification of apilimod as a first-in-class PIKfyve kinase inhibitor for treatment of B-cell non-Hodgkin lymphoma. Blood. 2017 Mar 30;129(13):1768-1778.

[2]Wada Y, Lu R, et al. Selective abrogation of Th1 response by STA-5326, a potent IL-12/IL-23 inhibitor. Blood. 2007;109(3):1156-64

[3]Cai X, Xu Y, Cheung AK, Tomlinson RC, Alcázar-Román A, Murphy L, Billich A, Zhang B, Feng Y, Klumpp M, Rondeau JM, Fazal AN, Wilson CJ, Myer V, Joberty G, Bouwmeester T, Labow MA, Finan PM, Porter JA, Ploegh HL, Baird D, De Camilli P, Tallarico JA, Huang Q. PIKfyve, a class III PI kinase, is the target of the small molecular IL-12/IL-23 inhibitor apilimod and a player in Toll-like receptor signaling. Chem Biol. 2013 Jul 25;20(7):912-21.

[4]Gayle S, Landrette S, Beeharry N, Conrad C, Hernandez M, Beckett P, Ferguson SM, Mandelkern T, Zheng M, Xu T, Rothberg J, Lichenstein H. Identification of apilimod as a first-in-class PIKfyve kinase inhibitor for treatment of B-cell non-Hodgkin lymphoma. Blood. 2017 Mar 30;129(13):1768-1778.