2. Protein Tyrosine Kinase/RTK MAPK/ERK Pathway Autophagy
  3. VEGFR PDGFR RET Raf c-Kit FGFR Autophagy Tie
  4. Regorafenib mesylate

Regorafenib mesylate  (Synonyms: BAY 73-4506 mesylate)

目录号: HY-10331B
产品使用指南

摩尔计算器

Regorafenib (BAY 73-4506) mesylate 是一种口服有效的多靶点受体酪氨酸激酶 (tyrosine kinase) 抑制剂，抑制 VEGFR1/2/3，PDGFRβ，Kit，RET 和 Raf-1 的 IC50 分别为 13/4.2/46，22，7，1.5 和 2.5 nM。Regorafenib mesylate 显示出非常强的抗肿瘤和抗血管生成活性。

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Regorafenib mesylate Chemical Structure

Regorafenib mesylate Chemical Structure

CAS No. : 835621-08-4

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Regorafenib mesylate 的其他形式现货产品:

Customer Review

Other Forms of Regorafenib mesylate:

Regorafenib mesylate 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 59 篇科研文献

WB

    Regorafenib mesylate purchased from MCE. Usage Cited in: Neoplasia. 2023 Mar 18;39:100897.  [Abstract]

    Regorafenib (0-40 µM; 36 h) markedly increases the expression of cleaved caspase-3, while decreases the expression of anti-apoptotic protein Bcl-2, in both H1299 and PC-9 cells.

    Regorafenib mesylate purchased from MCE. Usage Cited in: Int J Mol Sci. 2018 Sep 25;19(10). pii: E2915.  [Abstract]

    Effects on the expression of phosphorylated extracellular signal-related kinase (p-ERK), ERK, thymidylate synthase (TS), and markers of cell death in SW620, HCT 116, and HT-29 cells using various Regorafenib treatment schedules.

    Regorafenib mesylate purchased from MCE. Usage Cited in: Br J Cancer. 2017 Sep 26;117(7):974-983.  [Abstract]

    The effect of the AKT inhibitor MK2206 (10 μM) on the expression levels of phosphor-AKT, AKT, and STMN1 in TKI-pretreated NCI-H460 cells. β-actin is used as a loading control.

    查看 VEGFR 亚型特异性产品:

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    VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

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    PDGFR PDGFRβ PDGFRα

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    BRaf c-Raf Raf

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    FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

    查看 Tie 亚型特异性产品:

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    Tie2

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Regorafenib (BAY 73-4506) mesylate is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib mesylate shows very robust antitumor and antiangiogenic activity[1].

    IC50 & Target

    Tie2

    311 ± 46 nM (IC50)

    Raf-1

    2.5 ± 0.6 nM (IC50)

    VEGFR2

    4.2 ± 1.6 nM (IC50)

    VEGFR1

    13 ± 0.4 nM (IC50)

    BRafV600E

    19 ± 6 nM (IC50)

    PDGFRβ

    22 ± 3 nM (IC50)

    B-Raf

    28 ± 10 nM (IC50)

    VEGFR3

    46 ± 10 nM (IC50)

    体外研究
    (In Vitro)

    Regorafenib mesylate (0-10 μM, 96 h) shows anti-proliferation activity in GIST 882, Thyroid TT, MDA-MB-231, HepG2, A375 and SW620 cells[1].
    Regorafenib mesylate (0-3000 nM, 30 min) inhibits the autophosphorylation of VEGFR2, TIE2 and PDGFR-β, and inhibits FGFR and pERK1/2[1].
    Regorafenib mesylate causes a concentration-dependent decrease in Hep3B cell growth, with an IC50 of 5 μM. Regorafenib subsequently increases the levels of phospho-c-Jun, a JNK target, but not total c-Jun in Hep3B cells[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Regorafenib mesylate 相关抗体:

    Cell Proliferation Assay[1]

    Cell Line: GIST 882, Thyroid TT, MDA-MB-231, HepG2, A375 and SW620 cells
    Concentration: 10 μM and 5 nM
    Incubation Time: 96 h
    Result: Showed anti-proliferation activity in GIST 882, Thyroid TT, MDA-MB-231, HepG2, A375 and SW620 cells, with IC50 values of 45 ± 20, 34 ± 8, 401 ± 88, 560 ± 200, 900, 967 ± 287 nM. respectively.

    Western Blot Analysis[1]

    Cell Line: NIH-3T3/VEGFR2 cells, (CHO)-TIE2 cells, HAoSMCs cells, MCF-7 cells
    Concentration: 0, 10, 30, 100, 300, 1000, 3000 nM
    Incubation Time: 30 min
    Result: Inhibited the autophosphorylation of VEGFR2, TIE2 and PDGFR-β, with IC50 values of 3, 31, and 90 nM, respectively, inhibited FGFR signaling in MCF-7 breast cancer (BC) cells stimulated with FGF10, and showed inhibition of phosphorylated FGFR substrate 2 (pFRS2) and the downstream signaling kinase pERK1/2.
    体内研究
    (In Vivo)

    Regorafenib mesylate (10 mg/kg, Orally, single dose or daily for 4 days) inhibits tumor vasculature and tumor growth in a rat GS9L glioblastoma model[1].
    Regorafenib mesylate (0-100 mg/kg, Orally, qd × 9) exhibits antitumorigenic and antiangiogenic effects in the Colo-205, MDA-MB-231 and 786-O model[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Rat GS9L glioblastoma xenograft[1]
    Dosage: 10 mg/kg
    Administration: Orally, single dose or daily for 4 days
    Result: Inhibited tumor vasculature and tumor growth in a rat GS9L glioblastoma model.
    Animal Model: Female athymic NCr nu/nu mice, Multiple xenograft models, including models derived from CRC (Colo-205), BC (MDA-MB-231) and RCC (786-O) tumors[1]
    Dosage: 0, 3, 10, 30, 100 mg/kg
    Administration: Orally, qd × 9
    Result: Effectively inhibited growth of the Colo-205, MDA-MB-231 and 786-O model. Significantly reduces tumor MVA, effectively inhibited the RAF/MEK/ERK signaling cascade, and drastically inhibited tumor cell proliferation.
    Clinical Trial
    分子量

    578.92

    Formula

    C22H19ClF4N4O6S
    CAS 号
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    Please store the product under the recommended conditions in the Certificate of Analysis.
    纯度 & 产品资料
    参考文献

    Regorafenib mesylate 相关分类

    • 摩尔计算器

    • 稀释计算器

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Regorafenib835621-08-4BAY 73-4506VEGFRPDGFRRETRafc-KitFGFRAutophagyTieVascular endothelial growth factor receptorPlatelet-derived growth factor receptorRaf kinasesSCFRCD117Fibroblast growth factor receptorAngiopoietin receptorAntitumorigenicantiangiogenictumorHUVECsHep3B cellHAoSMCsNIH-3T3Colo-205MDA-MB-231786-OInhibitorinhibitorinhibit

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