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(Z)-LFM-A13
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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 Kis 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.
相关产品:Covalent Screening Library Plus | Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | Epigenetics Compound Library | Immunology/Inflammation Compound Library | JAK/STAT Compound Library | Kinase Inhibitor Library | Protein Tyrosine Kinase Compound Library | Stem Cell Signaling Compound Library | Anti-Cancer Compound Library | Anti-Aging Compound Library | Covalent Screening Library | Differentiation Inducing Compound Library | Reprogramming Compound Library | Anti-Breast Cancer Compound Library | Anti-Lung Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | Anti-Obesity Compound Library | Anti-Liver Cancer Compound Library | Anti-Prostate Cancer Compound Library | Cancer Stem Cells Compound Library | Membrane Protein-targeted Compound Library | Autoimmune Disease Compound Library | Serine/Threonine Kinase Inhibitor Library | AAPK-25 | JAK-IN-20 | Atuzabrutinib | JAK1-IN-9 | AT9283 | RO495 | TK4b | TAK-960 | JAK-IN-17 | (E/Z)-Zotiraciclib | Rigosertib sodium | JAK-IN-10 | PCI 29732 | (3R,4S)-Tofacitinib | JAK3/BTK-IN-6 | Tyk2-IN-5 | Pirtobrutinib | Brevilin A | CNX-500 | Broussonin E | Itacnosertib | BTK inhibitor 17 | RO8191 | Axltide | Fosifidancitinib | Remibrutinib | PLK1/BRD4-IN-1 | RN486 | JAK3-IN-6
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