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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-MEK (MAP2K)-KZ-001
KZ-001

Chemical Structure : KZ-001

CAS No.: 1448441-53-9

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KZ-001 (KZ001)

货号: PC-38901Not For Human Use, Lab Use Only.

KZ-001 is a highly potent and selective MEK 1/2 inhibitor with IC50 values of 7.4/64 nM, respectively, exhibits greater inhibition against BRAF- and KRAS-mutant tumor cells than AZD6244.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    KZ-001 is a highly potent and selective MEK1/2 inhibitor with IC50 values of 7.4/64 nM, respectively, exhibits greater inhibition against BRAF- and KRAS-mutant tumor cells than AZD6244.
    KZ-001 has approximately 27-fold stronger activity than AZD6244.
    KZ-001 (1 nM to 625 nM) inhibits cellular ERK phosphorylation in A375, Calu-6, Colo-205 and HT-29 cells.
    KZ-001 shows much more potent inhibition of proliferation, with an IC50 of 2.9-5.7 nM and 169.9 nM for the BRAFV600E and KRASQ61K cancer cell lines, compare with AZD6244, the RAFWT and RASWT cell lines A431 are resistant to KZ-001.
    KZ-001 induces apoptosis in Colo-205 and Calu-6 cells, but not RAFWT and RASWT cell lines. KZ-001 (3 mg/kg and 6 mg/kg) completely inhibits the growth of Colo-205 tumors (TGI 103.9% and 108.8%, respectively; p < 0.01).
    KZ-001 shows synergistic effect against BRAF mutant cell lines in vitro and in vivo, when combined with vemurafenib and docetaxel.

    物理化学性质&存储条件

    分子量 475.190
    分子式 C16H12F2IN3O4
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20°C 12 个月; 4°C 6 个月
    配置液
    -80°C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO
    Chemical Name/SMILES

    4-fluoro-5-((2-fluoro-4-iodophenyl)amino)-N-(2-hydroxyethoxy)benzo[d]oxazole-6-carboxamide

    参考文献

    1. Ying Cheng, et al. Int J Cancer. 2019 Jul 15;145(2):586-596.

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