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编 号：F407746
分子式：C11H8Br2N2O2
分子量：360
分子式：C11H8Br2N2O2
分子量：360
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CAS No: 62004-35-7
产品详情
生物活性：
LFM-A13 is a potent BTK, JAK2, PLK inhibitor, inhibits recombinant BTK, Plx1 and PLK3 with IC50s of 2.5 μM, 10 μM and 61 μM. LFM-A13 has antiproliferative activity and anticancer activity. LFM-A13 can be used in cancer-related research
体内研究：
LFM-A13 (10 或 50 mg/kg; 腹腔注射) 在 MMTV/Neu 转基因小鼠乳腺癌模型中表现出剂量依赖性的抗肿瘤作用。FM-A13 (50 mg/kg; 每周三次; 腹腔注射) 通过调节多种与细胞周期、存活和凋亡相关的因子，可减轻 DMBA 诱导的小鼠乳腺肿瘤发生。Animal Model:MMTV/neu transgenic mouse model
Dosage:50 or 100 mg/kg
Administration:Intraperitoneal injection (i.p.); twice a day for 5 consecutive days a week
Result:Attenuated mammary tumor formation in mice.
Animal Model:DMBA-induced breast cancer mouse model
Dosage:50 mg/kg (or combinated with Paclitaxel (HY-B0015) (10 mg/kg; once per week intraperitoneally))
Administration:Intraperitoneal injection (i.p.); 3 times a week
Result:Inhibited DMBA-induced mammary tumor incidence, average tumor number, average tumor weight, and size in BALB/c mice.Significantly decreased PLK1, cyclin D1, CDK-4, P53 and Bcl-2 expression, but increased the expression of p21, IκB, Bax and caspase 3 expression in mice.
体外研究：
LFM-A13 (100 μM; 4 h) 抑制 R10 细胞中 Epo 诱导的 EpoR、JAK2、BTK、STAT5和 ERK1/2 的磷酸化。LFM-A13 (100 μM; 转染 48 h) 抑制 COS 细胞中 JAK2，Tec 和 BTK 的自磷酸化，而不影响 Lyn 激酶自磷酸化。LFM-A13 有效抑制 Plx1，IC50 为 10 μM, 也抑制 BRK、BMX、FYN 和Met，IC50 分别为 267、281、240 和 215 μM。
LFM-A13 is a potent BTK, JAK2, PLK inhibitor, inhibits recombinant BTK, Plx1 and PLK3 with IC50s of 2.5 μM, 10 μM and 61 μM. LFM-A13 has antiproliferative activity and anticancer activity. LFM-A13 can be used in cancer-related research
体内研究：
LFM-A13 (10 或 50 mg/kg; 腹腔注射) 在 MMTV/Neu 转基因小鼠乳腺癌模型中表现出剂量依赖性的抗肿瘤作用。FM-A13 (50 mg/kg; 每周三次; 腹腔注射) 通过调节多种与细胞周期、存活和凋亡相关的因子，可减轻 DMBA 诱导的小鼠乳腺肿瘤发生。Animal Model:MMTV/neu transgenic mouse model
Dosage:50 or 100 mg/kg
Administration:Intraperitoneal injection (i.p.); twice a day for 5 consecutive days a week
Result:Attenuated mammary tumor formation in mice.
Animal Model:DMBA-induced breast cancer mouse model
Dosage:50 mg/kg (or combinated with Paclitaxel (HY-B0015) (10 mg/kg; once per week intraperitoneally))
Administration:Intraperitoneal injection (i.p.); 3 times a week
Result:Inhibited DMBA-induced mammary tumor incidence, average tumor number, average tumor weight, and size in BALB/c mice.Significantly decreased PLK1, cyclin D1, CDK-4, P53 and Bcl-2 expression, but increased the expression of p21, IκB, Bax and caspase 3 expression in mice.
体外研究：
LFM-A13 (100 μM; 4 h) 抑制 R10 细胞中 Epo 诱导的 EpoR、JAK2、BTK、STAT5和 ERK1/2 的磷酸化。LFM-A13 (100 μM; 转染 48 h) 抑制 COS 细胞中 JAK2，Tec 和 BTK 的自磷酸化，而不影响 Lyn 激酶自磷酸化。LFM-A13 有效抑制 Plx1，IC50 为 10 μM, 也抑制 BRK、BMX、FYN 和Met，IC50 分别为 267、281、240 和 215 μM。
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