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CAS No. : 1404095-34-6
MCE 国际站:CCT244747
产品活性:CCT244747 是一种有效的,可口服的,高度选择性的 CHK1 抑制剂,IC50 值为 7.7 nM;CCT244747 可废除 G2 检查点,IC50 值为 29 nM。
研究领域:Cell Cycle/DNA Damage
作用靶点:Checkpoint Kinase (Chk)
In Vitro: CCT244747 poorly inhibits CHK2 (IC50 >10 μM) and CDK1 (IC50 >10 μM). CCT244747 has potent activities against CHK1, RSK1, RSK2, AMPK, BRSK1, IRAK1,and TrkA, with >80% inhibition. CCT244747 (10 μM) exhibits <25% inhibition of the other ion channels including hNav1.5, hKv4.3/hKChIP2, hCav1.2, hKv1.5, hKCNQ1/hminK, hHCN4. CCT244747 inhibits FLT3 with an IC50 of 600 nM. CCT244747 (0.5 μM) overcomes genotoxic-induced S and G2 cell cycle arrest in human colon cancer cell lines. CCT244747 inhibits cellular CHK1 function with IC50s ranging from 29 nM to 170 nM for cellular G2 checkpoint abrogation (MIA, mitosis induction assay) in HT29, SW620, MiaPaCa-2, and Calu6 cell lines; the GI50s are between 0.33 and 3μM. CCT244747 (0.3 μM) inhibits SN38 and gemcitabine-induced CHK1 activity in HT29 and SW620 colon cancer cell lines and this correlates with abrogation of cell cycle arrest, induction of DNA damage and apoptosis. CCT244747 (0.5-2.0 μM) increases the sensitivity of bladder and head and neck cancer cell lines (T24, RT112 and Cal27) to radiation.
In Vivo: CCT244747 (100 mg/kg po, qd7d) significantly reduces tumor burden in human tumor xenografts. CCT244747 (100-300 mg/kg, po) inhibits gemcitabine-induced pS296 CHK1 for up to 24 h in HT29 colon tumor xenografts. CCT244747 (75 mg/kg, p.o.) in combination with gemcitabine has potent antitumor effects in HT29 colon tumor xenografts and Calu6 human lung cancer xenografts. CCT244747 (150 mg/kg p.o.) also shows antitumor activities with irinotecan in SW620 human colon tumor xenografts. CCT244747 (100 mg/kg, p.o.) exhibits radiosensitization activity in Cal27 xenografts.
相关产品:Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | Kinase Inhibitor Library | Anti-Cancer Compound Library | Anti-Aging Compound Library | Orally Active Compound Library | Chemical Probe Library | Anti-Lung Cancer Compound Library | Cancer Stem Cells Compound Library | Heterocyclic Compound Library | Highly Selective Inhibitors Library | SB-218078 | Chk2-IN-1 | BML-277 | Monalizumab | PV-1019 | MU380 | SCH900776 | PD 407824 | Prexasertib | GDC-0575 | CCT241533 dihydrochloride | GNE-900 | GDC-0425 | Chk1-IN-6 | CHK1-IN-2 | Zn-DPA-maytansinoid conjugate 1 | CCT245737 | CHK1-IN-3 | SAR-020106 | AZD-7762 hydrochloride | MRT00033659 | CHIR-124 | ANI-7 | VER-00158411 | CHK-IN-1 | CHK1-IN-4 | Chk1-IN-5
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货号: HY-18175
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