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| Cas No.: | 541550-19-0 |
| Chemical Name: | Apilimod |
| Synonyms: | Benzaldehyde,3-methyl-,2-[6-(4-morpholinyl)-2-[2-(2-pyridinyl)ethoxy]-4-pyrimidinyl]hydrazone;Apilimod;N-[(E)-(3-methylphenyl)methylideneamino]-6-morpholin-4-yl-2-(2-pyridin-2-ylethoxy)pyrimidin-4-amine;STA-5326;STA 5326;3-Methylbenzaldehyde [6-(4-morpholinyl)-2-[2-(2-pyridinyl)ethoxy]-4-pyrimidinyl]hydrazone;Kinome_3580;2-[2-(pyridin-2-yl)-ethoxy]-4-[n'-(3-methyl-benzilidene)-hydrazino]-6-(morpholin-4-yl)-pyrimidine;CID 49830988;APILIMOD;APILIMODUM;(E)-4-(6-(2-(3-methylbenzylidene)hydrazinyl)-2-(2-(pyridin-2-yl)ethoxy)pyrimidin-4-yl)morpholine;Sta 5326;Sta5326;Sta-5326;ApiliMod(STA5326);3-Methylbenzaldehyde 2-[6-(4-Morpholinyl)-2-[2-(2-pyridinyl)ethoxy]-4- pyriMidinyl]hydrazone;541550-19-0;BA177430;BDBM50590927;HY-14644;STA5326;EX-A908;NCGC00263093-14;GFW2K84S4L;BENZALDEHYDE, 3-METHYL-, 2-(6-(4-MORPHOLINYL)-2-(2-(2-PYRIDINYL)ETHOXY)-4-PYRIMIDINYL)HYDRAZONE;APILIMOD [WHO-DD];N-[6-Morpholin-4-yl-2-(2-pyridin-2-yl-ethoxy)-pyrimidin-4-yl]-N'-[1-m-tolyl-meth-(E)-ylidene]-hydrazine;BENZALDEHYDE, 3-METHYL-, (6-(4-MORPHOLINYL)-2-(2-(2-PYRIDINYL)ETHOXY)-4-PYRIMIDINYL)HYDRAZONE;s6414;DB05611;Apilimod [INN];CHEMBL4297643;NCGC00263093-02;AS-16828;SCHEMBL426299;Z2568726097;AKOS015909602;UNII-GFW2K84S4L;4-(6-(2-(3-Methylbenzylidene)hydrazinyl)-2-(2-(pyridin-2-yl)ethoxy)pyrimidin-4-yl)morpholine;N-(3-METHYL-BENZYLIDENE)-N'-(6-MORPHOLIN-4-YL-2-(2-PYRIDIN-2-YL-ETHOXY)-PYRIMIDIN-4-YL)-HYDRAZINE |
| SMILES: | O1C([H])([H])C([H])([H])N(C2C([H])=C(N([H])N=C([H])C3=C([H])C([H])=C([H])C(C([H])([H])[H])=C3[H])N=C(N=2)OC([H])([H])C([H])([H])C2=C([H])C([H])=C([H])C([H])=N2)C([H])([H])C1([H])[H] |
| Formula: | C23H26N6O2 |
| M.Wt: | 418.49 |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | Apilimod is a potent IL-12/IL-23 inhibitor, and strongly inhibits IL-12 with IC50s of 1 nM and 2 nM, in IFN-γ/SAC-stimulated human PBMCs and SAC-treated monkey PBMCs, respectively. |
| In Vivo: | Apilimod (10 mg/kg, p.o.) is effective not only when administered throughout the entire experiment, but also when administration is initiated on day 30 when disease is clearly measurable but not maximal. TA-5326 causes a significant reduction in cell number only in the Th1 model, with an average percentage of inhibition of 51%±8% relative to the vehicle control. Apilimod treatment has no effect in the Th2 setting[1]. Apilimod (5 or 20 mg/kg, p.o.) reduces the level of IL-12 p40 in serum without altering body weight in EAU mice. Oral administration of Apilimod reduces the severity of experimental autoimmune uveoretinitis (EAU) by clinical and histopathological analysis[2]. |
| In Vitro: | Apilimod inhibited IFN-γ production induced by either IFN-γ/SAC or SAC in human PBMCs, with an IC50 of approximately 20 nM. Apilimod show some inhibition against IFN-γ/SAC-induced TNF-α and ConA-induced IL-5 from human PBMCs at high concentrations, but no suppressive effect against IL-1β, IL-2, IL-4, IL-8, and IL-18 in all cultures tested. The p35 and p40 promoter-driven luciferase activities are significantly induced after stimulation with IFN-γ/LPS or IFN-γ/SAC, and are completely suppressed by 100 nM Apilimod[1]. |
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COA
| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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| 2018-0101 |
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