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PI-103
CAS No. 371935-74-9
PI-103 ( PI 103 | PI103 )
产品货号. M14282 CAS No. 371935-74-9
一种有效的 I 类 PI3K/mTOR 双抑制剂，p110α/β/δ/γ 的 IC50 分别为 2/3/3/15/。
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
| 5MG | ￥781 | 有现货 |
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| 10MG | ￥1216 | 有现货 |
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| 25MG | ￥1841 | 有现货 |
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| 50MG | ￥2678 | 有现货 |
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| 100MG | ￥3141 | 有现货 |
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| 200MG | ￥4473 | 有现货 |
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| 500MG | 获取报价 | 有现货 |
|
| 1G | 获取报价 | 有现货 |
|
| 1 mL x 10 mM in DMSO | ￥818 | 有现货 |
|
生物学信息
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产品名称PI-103
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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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产品简述一种有效的 I 类 PI3K/mTOR 双抑制剂，p110α/β/δ/γ 的 IC50 分别为 2/3/3/15/。
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产品描述A potent, dual class I PI3K/mTOR inhibitor with IC50 of 2/3/3/15/ for p110α/β/δ/γ, respectively; also inhibits TORC1 (>80% inhibition at 0.5 uM) and DNA-PK (IC50=14 nM), 15- to 20-fold less activity against class II PI3K C2β (IC50=43 nM), >1,300-fold selectivity over the class III PI3K Vsp34; potently inhibits proliferation and invasion of a wide variety of human cancer cells in vitro; shows activity in cancer xenograft models.
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体外实验PI-103 exhibits antiproliferative properties in a panel of human cancer cell lines. PI-103 is essentially cytostatic for cell lines and induced cell cycle arrest in the G1 phase. In blast cells, PI-103 inhibits leukemic proliferation, the clonogenicity of leukemic progenitors and induces mitochondrial apoptosis, especially in the compartment containing leukemic stem cells . PI-103 potently inhibits both the rapamycin-sensitive (mTORC1, IC50=20 nM) and rapamycin-insensitive (mTORC2, IC50=83 nM) complexes of the protein kinase mTOR.
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体内实验PI-103 shows therapeutic activity against a range of human tumor xenografts, exhibiting inhibition of angiogenesis, invasion, and metastasis, as well as direct antiproliferative effects. PI-103 induces immunosuppression promoting in vivo tumor growth and inhibiting apoptosis. Tumors from PI-103-treated mice shows higher levels of cyclin D1 and more proliferating cells.
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同义词PI 103 | PI103
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通路PI3K/Akt/mTOR signaling
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靶点PI3K
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受体DNA-PK|p110α|p110β|p110γ|p110δ|mTOR
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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 Number371935-74-9
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分子量348.3553
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分子式C19H16N4O3
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纯度>98% (HPLC)
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溶解度10 mM in DMSO
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SMILESOC1=CC(=CC=C1)C1=NC2=C(OC3=C2C=CC=N3)C(=N1)N1CCOCC1 |c:3,5,13,16,18,21,t:1,8,10|
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化学全称Phenol, 3-[4-(4-morpholinyl)pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]-
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. Fan QW, et al. Cancer Cell. 2006 May;9(5):341-9.
2. Raynaud FI, et al. Cancer Res. 2007 Jun 15;67(12):5840-50.
3. Fan QW, et al. Cancer Res. 2007 Sep 1;67(17):7960-5.
4. Kojima K, et al. Leukemia. 2008 Sep;22(9):1728-36.
产品手册
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