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SAR405
CAS No. 1523406-39-4
SAR405 ( SAR-405 | SAR 405 )
产品货号. M12127 CAS No. 1523406-39-4
SAR405 是一种高效、选择性 PI3K III 类亚型 Vps34 抑制剂，IC50 为 1.2 nM。
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
| 2MG | ￥583 | 有现货 |
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| 5MG | ￥851 | 有现货 |
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| 10MG | ￥1531 | 有现货 |
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| 25MG | ￥3062 | 有现货 |
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| 50MG | ￥4690 | 有现货 |
|
| 100MG | 获取报价 | 有现货 |
|
| 200MG | 获取报价 | 有现货 |
|
| 500MG | 获取报价 | 有现货 |
|
| 1G | 获取报价 | 有现货 |
|
生物学信息
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产品名称SAR405
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注意事项本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
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产品简述SAR405 是一种高效、选择性 PI3K III 类亚型 Vps34 抑制剂，IC50 为 1.2 nM。
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产品描述SAR405 is a highly potent and selective PI3K class III isoform Vps34 inhibitor with IC50 of 1.2 nM, inhibits the formation of autophagosomes in GFP-LC3 cells with IC50 of 4 nM; displays no activity against class I and II PI3K isoforms (IC50>10 uM), as well as PIKKs, ATM, ATR and DNA-PK, SMG1; affects both late endosome-lysosome compartments and prevents autophagy, shows synergistic antiproliferative activity in renal tumor cell lines combined with mTOR inhibitor everolimus; enhances the antitumor efficacy of cisplatin in mouse xenograft model of HNSCC.
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体外实验The activity of SAR405 is next evaluated on a dedicated Vps34 cellular assay using a GFP-FYVE–transfected HeLa cell line.SAR405 prevents autophagy and synergizes with mTOR inhibition in tumor cells. SAR405 prevents autophagosome formation with an IC50 of 42 nM. Treatment of starved cells with SAR405 completely inhibits the conversion to LC3-II in a dose-dependent manner. The effect of SAR405 on autophagy is then investigated. The GFP-LC3 model is used for the HTS and confirmed its activity on starved cells (IC50=419 nM). The conversion of LC3-I into LC3-II is also analyzed by western blotting on wild-type HeLa and H1299 cells.
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体内实验——
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同义词SAR-405 | SAR 405
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通路PI3K/Akt/mTOR signaling
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靶点PI3K
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受体PI3K
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研究领域Cancer
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适应症——
化学信息
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CAS Number1523406-39-4
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分子量443.8506
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分子式C19H21ClF3N5O2
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纯度>98% (HPLC)
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溶解度DMSO: ≥ 27 mg/mL
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SMILESO=C1C=C(N2[C@H](C)COCC2)N=C3N(CC4=CC(Cl)=CN=C4)[C@H](C(F)(F)F)CCN31
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化学全称4H-Pyrimido[1,2-a]pyrimidin-4-one, 9-[(5-chloro-3-pyridinyl)methyl]-6,7,8,9-tetrahydro-2-[(3R)-3-methyl-4-morpholinyl]-8-(trifluoromethyl)-, (8S)-
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1. Ronan B, et al. Nat Chem Biol. 2014 Dec;10(12):1013-9.
2. Pasquier B. Autophagy. 2015 Apr 3;11(4):725-6.
3. Valet C, et al. Blood. 2017 Nov 2;130(18):2032-2042.
4. New J, et al. Cancer Res. 2017 Dec 1;77(23):6679-6691.
产品手册
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