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LY364947 CAS NO.396129-53-6
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- Min.Order: 10 Gram
- Payment Terms: L/C
- Available Specifications:
≥98.0%(10-50)Gram≥98.0%(100-500)Gram
- Product Details
Keywords
- LY364947
- LY-364947;[3-(Pyridin-2-yl)-4-(4-quinonyl)]-1H-pyrazole;4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl]-quinoline;LY364947(HTS 466284);E 616451;HTS 466284;2-[4-(Quinolin-4-yl)-1H-pyrazol-3-yl]pyridine, 3-(Pyridin
- 396129-53-6
Quick Details
- ProName: LY364947
- CasNo: 396129-53-6
- Molecular Formula: C17H12N4
- Appearance: Light yellow transparent liquid
- Application: CAS：396129-53-6；
- DeliveryTime: 60days
- PackAge: 100mg/1g
- Port: shang hai
- ProductionCapacity: 10 Gram/Week
- Purity: 98%
- Storage: Dry seal
- Transportation: shipping
- LimitNum: 10 Gram
Superiority
We are specialized in custom synthesis, chemical/pharmaceutical/ pesticides outsourcing and contract research.
We are committed to provide excellence in researching, manufacturing and drug discovery process.
Our research team of scientists consists of western-trained Ph.D.s with experience and capabilities in drug R&D methodologies and medicinal chemistry.
Details
| LY 364947 |
| 生物活性 体外研究 体内研究 |
| 中文名称: | LY 364947 |
| 中文同义词: | 4-(3-吡啶-2-基-1H-吡唑-4-基)喹啉;4-[3-(2-吡啶基)-1H-吡唑-4-基]喹啉 |
| 英文名称: | LY-364947 |
| 英文同义词: | LY-364947;[3-(Pyridin-2-yl)-4-(4-quinonyl)]-1H-pyrazole;4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl]-quinoline;LY364947(HTS 466284);E 616451;HTS 466284;2-[4-(Quinolin-4-yl)-1H-pyrazol-3-yl]pyridine, 3-(Pyridin-2-yl)-4-(quinolin-4-yl)-1H-pyrazole;Quinoline, 4-[3-(2-pyridinyl)-1H-pyrazol-4-yl]- |
| CAS号: | 396129-53-6 |
| 分子式: | C17H12N4 |
| 分子量: | 272.31 |
| EINECS号: | |
| 相关类别: | API;小分子抑制剂;Inhibitors;小分子抑制剂，天然产物 |
| Mol文件: | 396129-53-6.mol |
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| LY 364947 性质 |
| 储存条件 | Store at RT |
| LY 364947 用途与合成方法 |
| 生物活性 | LY364947是一种有效的，ATP竞争性的TGFβR-I抑制剂，IC50为59 nM，比作用于TGFβR-II选择性高7倍。 |
| 体外研究 | LY364947 is an ATP competitive and tight-binding inhibitor, inhibiting phosphorylation of P-Smad3 by TGFβR-I kinase with Ki of 28 nM. LY364947 inhibits in vivo Smad2 phosphorylation within the NMuMg cells with IC50 of 135 nM. LY364947 reverses TGF-β-mediated growth inhibition in NMuMg cells with IC50 of 0.218 μM. LY364947 potentiates the xVent2-lux BMP4 response in NMuMg cells by 30% at concentrations as low as 0.25 μM. LY364947 (2 μM) prevents TGF-β-induced epithelial−mesenchymal transition in NMuMg cells. LY364947 (3 μM) induces expression of Prox1 and LYVE-1 in almost all HDLECs after 24 hours. LY364947 promotes nuclear export of Foxo3a, with low Smad2/3 and high Akt phosphorylation levels in leukaemia-initiating cells. LY364947 (< 20 μM) suppresses leukaemia-initiating cells colony-forming ability after co-culture with OP-9 stromal cells. |
| 体内研究 | LY364947 (1 mg/kg i.p.) accelerates lymphangiogenesis, as evidence by significantly increased the LYVE-1-positive areas, in a mouse model of chronic peritonitis. LY364947 (1 mg/kg i.p.) significantly increases the LYVE-1-positive areas in tumor tissues in tumor xenograft models using BxPC3 pancreatic adenocarcinoma cells. LY364947 (25 mg /kg) increases p-Akt and decreases nuclear Foxo3a in leukaemia-initiating cells in CML-affected mice. |