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簡(jiǎn)要描述：LY 294002是選擇性的, 可滲透細(xì)胞的特定PI3K抑制劑，可作用于酶的ATP結(jié)合位點(diǎn)，且抑制自體吞噬的螯合作用。在體內(nèi)，LY294002也抑制腫瘤生長(zhǎng)和誘導(dǎo)凋亡，尤其作用于LoVo腫瘤, 因此作用于鼠癌性腹膜炎模型具有明顯藥效。 LY294002明顯抑制卵巢癌生長(zhǎng)和腹水形成。
產(chǎn)品型號(hào)：abs810001a廠商性質(zhì)：生產(chǎn)廠家更新時(shí)間：2024-10-28訪 問 量：1227產(chǎn)品分類
Product Category詳細(xì)介紹
| 品牌 | absin | CAS | 154447-36-6 |
|---|---|---|---|
| 分子式 | - | 純度 | >98% |
| 分子量 | - | 貨號(hào) | abs810001 |
| 規(guī)格 | 10mg;25mg;100mg | 供貨周期 | 現(xiàn)貨 |
| 主要用途 | - | 應(yīng)用領(lǐng)域 | 生物產(chǎn)業(yè),綜合 |
| 產(chǎn)品描述 | |
| 描述 | LY 294002是已知抑制PI3Kα/δ/β的小分子，在無細(xì)胞測(cè)定中IC50分別為 0.5μM/0.57 μM/0.97μM；在溶液中比在Wortmannin中穩(wěn)定，也能夠阻斷自噬體的形成。
|
| 純度 | >98% |
| 儲(chǔ)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 | NSC 697286; SF 1101; LY 294002; LY-294002 |
| 外觀 | white to off-white powder |
| 可溶性/溶解性 | DMSO：36 mg/mL (117.13 mM) Ethanol：21 mg/mL (68.32 mM) |
| 生物活性 | |
| 靶點(diǎn) | p110α,p110δ,p110β,DNA-PK |
| In vitro(體外研究) | LY294002 is not exclusively selective for the PI3Ks, and could in fact act on other lipid kinases and additional apparently unrelated proteins. LY294002 is shown to inhibit not only mTOR and DNA-PK, but also other protein kinases, such as CK2 (casein kinase 2) and Pim-1. LY294002 inactivates Akt/PKB, consequently inhibiting cell proliferation and inducing apoptosis. LY294002 demonstrates a remarkable growth-inhibitory and apoptosis-inducing effect in these colon cancer cell lines, with decreased expression of phosphorylated Akt (Ser473). LY294002 induces marked nuclear pyknosis and diminished cytoplasmic volume in the tumor cells. Thus, LY294002 markedly inhibits ovarian cancer cell proliferation in vitro. LY294002 induces specific G1 arrest in cell growth, leading to almost complete inhibition of melanoma cell proliferation and partial inhibition of MG-63 (osteosarcoma cell line) proliferation. The effect of LY294002 on cell cycle progression may provide insights into a possible link between the PI3K activation pathway and cancer cell cycle regulation. |
| In vivo(體內(nèi)研究) | LY294002 also results in suppression of tumor growth and induction of apoptosis, especially in the LoVo tumors, and therefore shows remarkable effectiveness in the mouse peritonitis carcinomatosa model. LY294002 significantly inhibits growth and ascites formation of ovarian carcinoma. |
| 參考文獻(xiàn) | |
| 參考文獻(xiàn) | [1] Chaussade C, et al. Biochem J, 2007, 404(3), 449-58. [2] Semba S, et al. Clin Cancer Res, 2002, 8(6), 1957-63. [3] Hu L, et al. Clin Cancer Res, 2000, 6(3), 880-6. |
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