
簡要描述:Fimepinostat 1339928-25-4Fimepinostat potently inhibits class I PI3Ks as well as classes I and II HDAC enzymes.
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| 品牌 | absin | CAS | 1339928-25-4 |
|---|---|---|---|
| 分子式 | C23H24N8O4S | 純度 | ≥98% |
| 分子量 | 508.55 | 貨號 | abs47027893 |
| 規(guī)格 | 10mg | 供貨周期 | 現(xiàn)貨 |
| 主要用途 | potently inhibits class I PI3Ks | 應用領域 | 化工,生物產業(yè),農林牧漁,制藥/生物制藥,綜合 |
Fimepinostat 1339928-25-4
| 產品描述 | |
| 描述 | Fimepinostat potently inhibits class I PI3Ks as well as classes I and II HDAC enzymes. |
| 純度 | ≥98% |
| 儲存/保存方法 | Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 別名 | Fimepinostat;PI3K/HDAC Inhibitor |
| 可溶性/溶解性 | DMSO : ≥ 50 mg/mL (98.32 mM) |
| 生物活性 | |
| 靶點 | HDAC1,HDAC3,HDAC10,HDAC2,HDAC11 |
| In vitro(體外研究) | CUDC-907 inhibits other PI3K isoforms such as PI3Kβ, PI3Kγ, PI3Kδ, PI3KɑH1047R and PI3KɑE545K with IC50 of 54 nM, 311 nM, 39 nM, 73 nM and 62 nM, respectively. Moreover, CUDC-907 also prevents HDAC subtypes HDAC8, HDAC6 and HDAC11 with IC50 of 191 nM, 27 nM and 5.4 nM, respectively. In addition, CUDC-907 suppresses other types of HDAC enzymatic activity with lower potency. CUDC-907 inhibits the growth of a series of B cell lymphoma such as Granta 519, DOHH2, RL, Pfeiffer, SuDHL4, Daudi and Raji with IC50 of 7 nM, 1 nM, 2 nM, 4 nM, 3 nM, 15 nM and 9 nM, respectively. CUDC-907 also blocks the proliferation of Myeloma including RPMI8226, OPM-2 and ARH77 with IC50 of 2 nM, 1 nM and 5 nM, respectively. CUDC-907 displays greater anti-tumor activity in multiple myeloma and B cell lymphoma. |
| In vivo(體內研究) | CUDC-907 has a long half-life in murine tumors. CUDC-907 induces apoptosis and inhibits cancer cell proliferation in xenograft tumors. In efficacy studies in NHL and MM models, CUDC-907 is more efficacious than either a single-agent PI3K or HDAC inhibitor reference compound or a combination of the two agents given at maximally tolerated doses (MTD). Furthermore, CUDC-907 is more efficacious than the PI3Kδ-selective inhibitor CAL-101 when dosed at MTD doses. |
| 研究領域 | |
| 研究領域 | CardiovascularHeartHypertrophyOther EpigeneticsChromatin Modifying EnzymesAcetylation EpigeneticsChromatin Modifying EnzymesAcetylationHDACsClass I Stem CellsSignaling PathwaysWntHDACs Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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