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(Z)-LFM-A13

CAS No. : 244240-24-2

MCE 站：(Z)-LFM-A13

产品活性：LFM-A13 是一种有效的 BTK，JAK2，PLK 抑制剂，可抑制 BTK，Plx1 和 PLK3 的活性，IC₅₀ 分别为 2.5 μM，10 μM 和 61 μM。

研究领域：Protein Tyrosine Kinase/RTK  |  Cell Cycle/DNA Damage  |  Epigenetics  |  Stem Cell/Wnt  |  JAK/STAT Signaling

作用靶点：Btk  |  Polo-like Kinase (PLK)  |  JAK

In Vitro: LFM-A13 significantly inhibits BTK activity with an IC₅₀ of 6.2 ± 0.3 μg/mL (= 17.2 ± 0.8 μM). The calculated K_is of LFM-A13 for BTK, JAK1, JAK3, IRK, EGFR ａnd HCK are 1.4, 110, 148, 31.6, 166 ａnd 214 μM. LFM-A13 (200 μM) markedly increases the chemosensitivity of ALL-1 cells to ceramide-induced apoptosis. LFM-A13 (100 μM) suppresses Epo-induced phosphorylation of EpoR, Jak2, Btk, Stat5 ａnd Erk1/2 in R10 cells. LFM-A13 (100 μM) inhibits auto-phosphorylation of Jak2, Tec ａnd Btk rather than Lyn kinase auto-phosphorylation in COS cells. LFM-A13 potently inhibits Plx1 with IC₅₀ of 10 μM; also inhibits BRK, BMX, FYN ａnd with IC₅₀s of 267, 281, 240 ａnd 215 μM.

In Vivo: LFM-A13 (25, 50 ａnd 100 mg/kg) shows no apparent toxicity to rats. LFM-A13 (50 mg/kg, three times a week, i.p.) attenuates mammary tumorigenesis in mice. LFM-A13 alone or in combination with paclitaxel shows marked effect on the breast tumor incidence, mean tumor numbers, average tumor weight, ａnd size in BALB/c mice. LFM-A13 (50 mg/kg, three times a week, i.p.) significantly decreases PLK1, cyclin D1, CDK-4, P53 ａnd Bcl-2 expression, but increases the expression of p21, IκB, Bax ａnd caspase 3 expression in mice. LFM-A13 (200 mg/kg) does not cause hematologic toxicity in rats. LFM-A13 (10 or 50 mg/kg, i.p.) exhibits anti-tumor effects dose dependently in the MMTV/Neu transgenic mouse model of breast cancer.

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