- ￥600 - 3200
- 上海莼试
- CS-01Y66297
- 国产
- 2025年07月13日
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- 详细信息
- 技术资料
- 库存：
34
- 英文名：
PND-1186
- CAS号：
1061353-68-1
- 供应商：
上海莼试
- 保存条件：
Store at -20°C
- 规格：
10mM (in 1mL DMSO) 5mg 10mg 50mg 100mg
使用方法：
1.本蛋白酶抑制剂混合物为100×的储存液，使用时按照1:100的比例加入到裂解液中(例如，1ml裂解液中加入10μl蛋白酶抑制剂混合物)，混匀后即可使用。根据需要，0.5M的EDTA也按照1:100的比例加入到裂解液中（如用于检测金属蛋白酶活性，则不宜添加EDTA）。含有蛋白酶抑制剂混合物的裂解液宜现用现配，不宜配制后冻存待后续使用。
2. 待所需的抑制剂添加完毕混匀后，就可以开始进行哺乳动物组织的裂解和蛋白提取。
商品属性：
产品描述：
分子式:C25H26F3N5O3
分子量:501.5
溶解度:≥ 50.2 mg/mL in DMSO
储存条件:Store at -20°C
General tips:For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition:Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
PND-1186 is a reversible inhibitor of FAK (focal adhesion kinase) with IC50 value of 1.5 nM [1].The cytoplasmic protein-tyrosine kinase FAK is associated with integrins and growth factor receptors. It modulates a variety of cellular processes when it is activated. Since the elevated expression of FAK is found in many tumors, the inhibitors of FAK are developed as anti-tumor drugs in cancer therapy. PND-1186 is one of these ATP-competitive small-molecule inhibitors. It inhibited the autophosphorylation of FAK tyrosine-397 with IC50 value of 0.1 μM in breast carcinoma cells. When the concentration was up to 1 μM, PND-1186 also inhibited more than 50% of the activities of other kinases, such as CDK2, Lck, Aurora-A and ACK1 [1].PND-1186 at concentrations of 0.1 to 1 μM inhibited the phosphorylation of FAK Tyr-397 and increased the protein level of FAK in murine breast carcinoma 4T1 cells, ID8 ovarian carcinoma cells and human MD-MBA-231 cells. Meanwhile, PND-1186 significantly induced cell apoptosis and increased the cleavage caspase 3 in suspended but not adherent 4T1 cells. Besides that, PND-1186 is found to inhibit the movement of 4T1 cells in both the wound healing assays and the millicell chamber motility assays. Treatment of PND-1186 at 0.4 μM for 4 hours showed the maximal inhibition of about 60%. In HEY ovarian cancer cells, treatment of PND-1186 caused the decrease of pY397 FAK, β5 integrin and osteopontin. It also induced cell cycle arrest at G0-G1 phase [1, 2].In subcutaneous 4T1 tumors, administration of PND-1186 at dose of 100 mg/kg caused inhibition of both FAK Tyr-397 phosphorylation and p130Cas Tyr-410 phosphorylation. In orthotopic 4T1 tumors, administration of 150 mg/kg PND-1186 for 16 days finally reduced 3.1-fold tumor volume. Moreover, PND-1186 is reported to have anti-inflammatory effects and can suppress the processes of spontaneous breast cancer metastasis to lung [3].
注意事项：
抗逆滴加序列
每次向板内滴加抗原时，移液器滴头要与平面45度悬空，不要触碰到孔内的液体，由后向前依次滴加(即浓度由低往高滴加)。
抗感染反应期
抗原抗体在室温20~25℃下，必须反应30min以上，若环境温度低于室温，可将微量反应板置于恒温培养箱中，使二者充分反应。
旅游温度
磷酸盐缓冲液的pH值要在高压灭菌后进行滴定，往往在高压后pH值会有所改变，所以高压后再调一次pH值更为准确。磷酸盐缓冲液一经使用保存期不要超过3周。当pH<5.8时，红细胞会产生自凝现象;当pH>7.8时，图形洗脱加快，易造成肉眼观察产生误差;p H=7.2时，红细胞沉降最充分，图形最清晰。
当滴注 1%红细胞悬液时，应经常摇晃红细胞悬液，使红细胞均匀地分布在磷酸缓冲液中，以防止红细胞下降。
反应时间及温度
加入鸡红血球之后，反应板在室温(20~25℃)静置30~40min，对照孔血球下沉于孔底，即可判定结果。若室温达不到实验要求，需相应调整反应时间。当环境温度低于4℃时，红细胞发生自凝;高于37℃时，会发生反应物分离和红细胞溶血。
公司正在出售的产品：
1.本蛋白酶抑制剂混合物为100×的储存液，使用时按照1:100的比例加入到裂解液中(例如，1ml裂解液中加入10μl蛋白酶抑制剂混合物)，混匀后即可使用。根据需要，0.5M的EDTA也按照1:100的比例加入到裂解液中（如用于检测金属蛋白酶活性，则不宜添加EDTA）。含有蛋白酶抑制剂混合物的裂解液宜现用现配，不宜配制后冻存待后续使用。
2. 待所需的抑制剂添加完毕混匀后，就可以开始进行哺乳动物组织的裂解和蛋白提取。
商品属性：
| 货号 | CS-01Y66297 | 规格 | 10mM (in 1mL DMSO) 5mg 10mg 50mg 100mg |
| CAS号 | 1061353-68-1 | 分子量 | 501.5 |
| 含量 | >98.00% | 别名 | SR-2516;PND 1186;PND1186;SR 2516;SR2516; VS-4718; VS 4718; VS4718 |
| 分子式 | C25H26F3N5O3 | 化学名 | |
| 产地 | 国产 | 用途 | 仅供科研研究实验 |
分子式:C25H26F3N5O3
分子量:501.5
溶解度:≥ 50.2 mg/mL in DMSO
储存条件:Store at -20°C
General tips:For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition:Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
PND-1186 is a reversible inhibitor of FAK (focal adhesion kinase) with IC50 value of 1.5 nM [1].The cytoplasmic protein-tyrosine kinase FAK is associated with integrins and growth factor receptors. It modulates a variety of cellular processes when it is activated. Since the elevated expression of FAK is found in many tumors, the inhibitors of FAK are developed as anti-tumor drugs in cancer therapy. PND-1186 is one of these ATP-competitive small-molecule inhibitors. It inhibited the autophosphorylation of FAK tyrosine-397 with IC50 value of 0.1 μM in breast carcinoma cells. When the concentration was up to 1 μM, PND-1186 also inhibited more than 50% of the activities of other kinases, such as CDK2, Lck, Aurora-A and ACK1 [1].PND-1186 at concentrations of 0.1 to 1 μM inhibited the phosphorylation of FAK Tyr-397 and increased the protein level of FAK in murine breast carcinoma 4T1 cells, ID8 ovarian carcinoma cells and human MD-MBA-231 cells. Meanwhile, PND-1186 significantly induced cell apoptosis and increased the cleavage caspase 3 in suspended but not adherent 4T1 cells. Besides that, PND-1186 is found to inhibit the movement of 4T1 cells in both the wound healing assays and the millicell chamber motility assays. Treatment of PND-1186 at 0.4 μM for 4 hours showed the maximal inhibition of about 60%. In HEY ovarian cancer cells, treatment of PND-1186 caused the decrease of pY397 FAK, β5 integrin and osteopontin. It also induced cell cycle arrest at G0-G1 phase [1, 2].In subcutaneous 4T1 tumors, administration of PND-1186 at dose of 100 mg/kg caused inhibition of both FAK Tyr-397 phosphorylation and p130Cas Tyr-410 phosphorylation. In orthotopic 4T1 tumors, administration of 150 mg/kg PND-1186 for 16 days finally reduced 3.1-fold tumor volume. Moreover, PND-1186 is reported to have anti-inflammatory effects and can suppress the processes of spontaneous breast cancer metastasis to lung [3].
注意事项：
抗逆滴加序列
每次向板内滴加抗原时，移液器滴头要与平面45度悬空，不要触碰到孔内的液体，由后向前依次滴加(即浓度由低往高滴加)。
抗感染反应期
抗原抗体在室温20~25℃下，必须反应30min以上，若环境温度低于室温，可将微量反应板置于恒温培养箱中，使二者充分反应。
旅游温度
磷酸盐缓冲液的pH值要在高压灭菌后进行滴定，往往在高压后pH值会有所改变，所以高压后再调一次pH值更为准确。磷酸盐缓冲液一经使用保存期不要超过3周。当pH<5.8时，红细胞会产生自凝现象;当pH>7.8时，图形洗脱加快，易造成肉眼观察产生误差;p H=7.2时，红细胞沉降最充分，图形最清晰。
当滴注 1%红细胞悬液时，应经常摇晃红细胞悬液，使红细胞均匀地分布在磷酸缓冲液中，以防止红细胞下降。
反应时间及温度
加入鸡红血球之后，反应板在室温(20~25℃)静置30~40min，对照孔血球下沉于孔底，即可判定结果。若室温达不到实验要求，需相应调整反应时间。当环境温度低于4℃时，红细胞发生自凝;高于37℃时，会发生反应物分离和红细胞溶血。
公司正在出售的产品：
| 辣根过氧化物酶标记的兔抗生物素抗体IgG H&L | Alexa Fluor 350标记的羊抗小鼠IgG H&L |
| 罗丹明标记的小鼠抗大鼠IgG H&L | 周期素依赖性激酶5调节蛋白1样蛋白1抗体 |
| PE标记的羊抗兔IgG H&L | MYC启动子结合蛋白1抗体 |
| Cy7标记的兔抗猴IgG H&L | 碱性磷酸酶(类胎盘型)抗体 |
| PE-CY5标记的小鼠抗兔IgG H&L | 跨膜蛋白SEMA5A抗体 |
| AF405标记的山羊抗兔IgG (H&L) | 磷酸化表皮生长因子受体抗体 |
| PE-CY5标记的兔抗猴IgM | 金属蛋白酶相关蛋白1抗体 |
| APC标记的羊抗鸡IgG H&L | 细胞色素b5还原酶3抗体 |
| Alexa Fluor 594标记的羊抗小鼠IgM | I型胶原蛋白 |
| APC标记的兔抗猴IgM | 磷酸化非受体性蛋白酪氨酸激酶ETK抗体 |
| Alexa Fluor 555标记的兔抗狗IgG H&L | CD20单克隆抗体 |
| Cy5.5标记的兔抗犬IgM抗体 | 特异性囊肿病液体蛋白15 |
| 辣根过氧化物酶标记的羊抗鸡IgG H&L | PND-1186MHC I类链相关蛋白A/组织相容性复合物MHCIa抗体 |
| 泛素羧基端酯酶L5(UCHL5)重组蛋白 | RNA结合蛋白34抗体 |
| 微管蛋白β3抗体 | 上皮细胞粘附分子（CD326）抗体 |
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PND-1186
￥600 - 3200
