化合物PND-1186 T1950
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Product IntroductionBioactivity英文名: PND-1186描述: PND-1186 (VS-4718) 是一种高特异性的FAK 可逆抑制剂，IC50为 1.5 nM。它选择性促进肿瘤细胞凋亡。细胞实验: For
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Product Introduction
Bioactivity
英文名: PND-1186
描述: PND-1186 (VS-4718) 是一种高特异性的FAK 可逆抑制剂，IC50为 1.5 nM。它选择性促进肿瘤细胞凋亡。
细胞实验: For soft agar assays, 48-well plates are coated with a 1:4 mix of 2% agar (EM Science) in 0.2 mL growth media (bottom layer). 5×104 cells are plated per well (in triplicate) in a mixture of 0.3% agar in 0.2 mL growth media (top layer). After agar solidification, 0.2 mL growth media is added containing DMSO or PND-1186 (final concentration for 0.6 mL). In separate experiments, PND-1186 is added after 4 days. After 10 days, colonies are imaged in phase contrast, enumerated by counting 9 fields (3 fields per well), and total area determined using Image J. For all analyses, experimental points are performed in triplicate and repeated at least two times. (Only for Reference)
激酶实验: In vitro kinase activity: GST-FAK in vitro kinase activity is measured and compared to His-tagged FAK 411–686 using the K-LISA screening kit and poly(Glu:Tyr) (4:1) copolymer as a substrate immobilized on microtiter plates. IC50 values are determined with various concentrations of test compounds in a buffer containing 50 μM ATP and 10 mM MnCl2, 50 mM HEPES (pH 7.5), 25 mM NaCl, 0.01% BSA, and 0.1 mM Na orthovanadate for 5 min at room temperature. Serial diluted compounds are tested in triplicate. Substrate phosphorylation is measured using horseradish peroxidase-conjugated anti-pTyr antibodies with spetrophotometric color quantitation. IC50 values are determined using the Hill-Slope Model. Kinase selectivity profiling is performed by using the KinaseProfiler service.
体外活性: 在负荷4T1肿瘤的小鼠体内,PND-1186（100 mg/kg,s.c.）可诱导细胞凋亡,对4T1皮下肿瘤生长产生抑制作用.在负荷ID8肿瘤的小鼠体内,PND-1186（0.5 mg/mL,p.o.）还会抑制卵巢癌肿瘤的生长.
体内活性: 在体外,PND-1186对4T1乳腺癌能动性有抑制作用,且可促进悬浮状态的4T1凋亡,并使4T1软琼脂集落数量和大小减少。在HEY 和 OVCAR8细胞中,PND-1186促使G0-G1细胞周期阻滞,从而使细胞死亡。
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 23 mg/mL (45.9 mM)
关键字: tumor | integrin | PTK2 | inhibit | Apoptosis | growth | Focal adhesion kinase | FAK | PTK2 protein tyrosine kinase 2 | PND-1186 | VS4718 | SR2516 | SR 2516 | survival | Inhibitor | cell | VS 4718
相关产品: GSPT1 degrader-1 | (E)-Flavokawain A | Barasertib | Hesperetin | Quiflapon | Thrombospondin-1 (1016-1023) (human, bovine, mouse) | (-)-Anonaine | Diclofenac | MARK4 inhibitor 1 | NM-3
相关库: Drug Repurposing Compound Library | Anti-Cancer Drug Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Active Compound Library | Tyrosine Kinase Inhibitor Library | Apoptosis Compound Library | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library
Bioactivity
英文名: PND-1186
描述: PND-1186 (VS-4718) 是一种高特异性的FAK 可逆抑制剂，IC50为 1.5 nM。它选择性促进肿瘤细胞凋亡。
细胞实验: For soft agar assays, 48-well plates are coated with a 1:4 mix of 2% agar (EM Science) in 0.2 mL growth media (bottom layer). 5×104 cells are plated per well (in triplicate) in a mixture of 0.3% agar in 0.2 mL growth media (top layer). After agar solidification, 0.2 mL growth media is added containing DMSO or PND-1186 (final concentration for 0.6 mL). In separate experiments, PND-1186 is added after 4 days. After 10 days, colonies are imaged in phase contrast, enumerated by counting 9 fields (3 fields per well), and total area determined using Image J. For all analyses, experimental points are performed in triplicate and repeated at least two times. (Only for Reference)
激酶实验: In vitro kinase activity: GST-FAK in vitro kinase activity is measured and compared to His-tagged FAK 411–686 using the K-LISA screening kit and poly(Glu:Tyr) (4:1) copolymer as a substrate immobilized on microtiter plates. IC50 values are determined with various concentrations of test compounds in a buffer containing 50 μM ATP and 10 mM MnCl2, 50 mM HEPES (pH 7.5), 25 mM NaCl, 0.01% BSA, and 0.1 mM Na orthovanadate for 5 min at room temperature. Serial diluted compounds are tested in triplicate. Substrate phosphorylation is measured using horseradish peroxidase-conjugated anti-pTyr antibodies with spetrophotometric color quantitation. IC50 values are determined using the Hill-Slope Model. Kinase selectivity profiling is performed by using the KinaseProfiler service.
体外活性: 在负荷4T1肿瘤的小鼠体内,PND-1186（100 mg/kg,s.c.）可诱导细胞凋亡,对4T1皮下肿瘤生长产生抑制作用.在负荷ID8肿瘤的小鼠体内,PND-1186（0.5 mg/mL,p.o.）还会抑制卵巢癌肿瘤的生长.
体内活性: 在体外,PND-1186对4T1乳腺癌能动性有抑制作用,且可促进悬浮状态的4T1凋亡,并使4T1软琼脂集落数量和大小减少。在HEY 和 OVCAR8细胞中,PND-1186促使G0-G1细胞周期阻滞,从而使细胞死亡。
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 23 mg/mL (45.9 mM)
关键字: tumor | integrin | PTK2 | inhibit | Apoptosis | growth | Focal adhesion kinase | FAK | PTK2 protein tyrosine kinase 2 | PND-1186 | VS4718 | SR2516 | SR 2516 | survival | Inhibitor | cell | VS 4718
相关产品: GSPT1 degrader-1 | (E)-Flavokawain A | Barasertib | Hesperetin | Quiflapon | Thrombospondin-1 (1016-1023) (human, bovine, mouse) | (-)-Anonaine | Diclofenac | MARK4 inhibitor 1 | NM-3
相关库: Drug Repurposing Compound Library | Anti-Cancer Drug Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Active Compound Library | Tyrosine Kinase Inhibitor Library | Apoptosis Compound Library | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library
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