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- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
PP121
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
1092788-83-4
- 规格：
100mg/50mg/25mg/10mg/1mg/5mg
| 规格： | 100mg | 产品价格： | ￥3940.0 |
|---|---|---|---|
| 规格： | 50mg | 产品价格： | ￥2966.0 |
| 规格： | 25mg | 产品价格： | ￥1680.0 |
| 规格： | 10mg | 产品价格： | ￥828.0 |
| 规格： | 1mg | 产品价格： | ￥340.0 |
| 规格： | 5mg | 产品价格： | ￥514.0 |
| 基本信息 | |
| CAS | No.1092788-83-4 |
| 英文名称 | PP121 |
| 分子式 | C17H17N7 |
| 分子量 | 319.36 |
| 溶解性 | Soluble in DMSO ≥2mg/mL(Need ultrasonic) |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL | MFCD12912434 |
| SMILES | C1CCC(C1)N2C3=NC=NC(=C3C(=N2)C4=CN=C5C(=C4)C=CN5)N |
| InChIKey | NVRXTLZYXZNATH-UHFFFAOYSA-N |
| InChI | InChI=1S/C17H17N7/c18-15-13-14(11-7-10-5-6-19-16(10)20-8-11)23-24(12-3-1-2-4-12)17(13)22-9-21-15/h5-9，12H，1-4H2，(H，19，20)(H2，18，21，22) |
| PubChem CID | 24905142 |
| 靶点 | mTOR;DNK-PK;VEGFR2;Src;PDGFR |
| 通路 | PI3K/Akt/mTOR;DNA Damage/DNA Repair;Angiogenesis; Protein Tyrosine Kinase/RTK |
| 背景说明 | PP121是多靶点激酶抑制剂，抑制 mTOR，DNK-PK，VEGFR2，Src，PDGFR。 |
| 生物活性 | PP121 is a multi-targeted kinase inhibitor with IC50s of 10， 60， 12， 14， 2 nM for mTOR， DNK-PK， VEGFR2， Src， PDGFR， respectively.[1-2] |
| In Vitro | PP121 blocks the PI3K pathway by direct inhibition of PI3K/mTOR in two glioblastoma cell lines， U87 and LN229. PP121 potently inhibits the proliferation of a diverse panel of tumor cell lines containing mutations in the PI3-K pathway components PIK3CA， PTEN， or RAS. PP121 induces a G0G1 arrest in most tumor cells. PP121 directly inhibits Src in cells and reverses its biochemical and morphological effects. PP121 potently inhibits the Ret kinase domain in vitro (IC50VEGF stimulated activation of the PI3-K and MAPK pathways. PP121 inhibits VEGFR2 autophosphorylation at low nanomolar concentrations， confirming that this molecule directly targets VEGFR2 in cells. PP121 inhibits Bcr-Abl induced tyrosine phosphorylation in K562 cells as well as BaF3 cells that express Bcr-Abl[1]. |
| 细胞实验 | Oral administration of PP121 remarkably inhibits Eca-109 xenograft growth. Mice body weights are not significantly affected by PP121 or the vehicle treatment. PP121 oral administration dramatically inhibits activations of Akt-mTOR and NFkB in xenograft tumors. p-Akt Ser 473 and p-IKKa/b are both inhibited by PP121 administration[2]. |
| 细胞实验 | Cells grown in 96-well plates are treated with PP121 at 4-fold dilutions (10 μM - 0.040 μM) or vehicle (0.1% DMSO). After 72 h cells are exposed to Resazurin sodium salt (22 μM) and fluorescence is quantified. IC50 values are calculated. For proliferation assays involving single cell counting， non-adherent cells are plated at low density (3–5% confluence) and treated with drug (2.5 μM) or vehicle (0.1% DMSO). Cells are diluted into trypan blue daily and viable cells counted using a hemocytometer[1]. |
| 动物实验 | Mice: Eca-109 cells are injected into the axillary regions of nude mice (5×106 cells/mouse). When the tumor volumes reach around 200 mm3， the mice are randomly separated to three groups: Untreated control， PP121 (30 mg/kg) and vehicle (10% 1-methyl-2-pyrrolidinone and 90% PEG 300) group. Tumor volumes and the mice body weights are measured every 10 d[2]. |
| 激酶实验 | Purified kinase domains are incubated with inhibitors (PP121) at 2- or 4-fold dilutions over a concentration range of 50- 0.001 μM or with vehicle (0.1% DMSO) in the presence of 10 μM ATP， 2.5 μCi of γ- 32P-ATP and substrate. Reactions are terminated by spotting onto nitrocellulose or phosphocellulose membranes， depending on the substrate; this membrane is then washed 5-6 times to remove unbound radioactivity and dried. Transferred radioactivity is quantitated by phosphorimaging and IC50 values are calculated by fitting the data to a sigmoidal doseresponse using Prism software[1]. |
| 数据来源文献 | [1]. Apsel B， et al. Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol， 2008， 4(11)， 691-699. [2]. Peng Y， et al. The anti-esophageal cancer cell activity by a novel tyrosine/phosphoinositide kinase inhibitor PP121. Biochem Biophys Res Commun. 2015 Sep 11;465(1):137-44. |
| 单位 | 瓶 |
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