2. Protein Tyrosine Kinase/RTK Autophagy MAPK/ERK Pathway
  3. VEGFR Autophagy PDGFR Raf RET
  4. Regorafenib Hydrochloride

Regorafenib Hydrochloride  (Synonyms: BAY 73-4506 hydrochloride)

製品番号: HY-13308 純度: 99.09%
COA 取扱説明書 Technical Support

Regorafenib Hydrochloride (BAY 73-4506 hydrochloride) is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.

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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号 : 835621-07-3

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 43 在庫あり
Solution
10 mM * 1 mL in DMSO USD 43 在庫あり
Solid
5 mg $38 在庫あり
10 mg $60 在庫あり
50 mg $120 在庫あり
100 mg $180 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 87 publication(s) in Google Scholar

Other Forms of Regorafenib Hydrochloride:

Regorafenib Hydrochloride 関連抗体

Top Publications Citing Use of Products

顧客検証

WB

    Regorafenib Hydrochloride purchased from MedChemExpress. Usage Cited in: Neoplasia. 2023 May: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 Hydrochloride purchased from MedChemExpress. 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 Hydrochloride purchased from MedChemExpress. 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.

    VEGFR アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

    PDGFR アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    PDGFR PDGFRβ PDGFRα

    Raf アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    B-Raf C-Raf Raf

    • 生物活性

    • プロトコル

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    Regorafenib Hydrochloride (BAY 73-4506 hydrochloride) is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively[1].

    IC50 & Target[1]

    VEGFR1

    13 nM (IC50)

    VEGFR2

    4.2 nM (IC50)

    VEGFR3

    46 nM (IC50)

    PDGFRβ

    22 nM (IC50)

    Braf

    28 nM (IC50)

    BRafV600E

    19 nM (IC50)

    Raf-1

    2.5 nM (IC50)

    体外実験

    Regorafenib potently inhibits VEGFR2 autophosphorylation in NIH-3T3/VEGFR2 cells with an IC50 of 3 nM. In HAoSMCs, regorafenib inhibits PDGFR-β autophosphorylation after stimulation with PDGF-BB, with an IC50 of 90 nM. Regorafenib inhibits the proliferation of VEGF165-stimulated HUVECs, with an IC50 of 3 nM[1]. Regorafenib causes a concentration-dependent decrease in Hep3B cell growth, having 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[3].

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

    Regorafenib Hydrochloride 関連抗体
    体内実験

    Regorafenib effectively inhibits growth of the Colo-205 xenografts in the dose range of 10-100 mg/kg reaching a TGI of 75% at day 14 at the 10 mg/kg dose. In the MDA-MB-231 model, regorafenib is highly efficacious at a dose as low as 3 mg/kg, resulting in a significant TGI of 81%, which increases to 93% at doses of 10 and 30 mg/kg, where tumor stasis is reached[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    分子量

    519.28

    分子式

    C21H16Cl2F4N4O3
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    ClC1=C(C(F)(F)F)C=C(NC(NC2=C(F)C=C(OC3=CC=NC(C(NC)=O)=C3)C=C2)=O)C=C1.Cl
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
    溶剤 & 溶解度
    体外: 

    DMSO : 100 mg/mL (192.57 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9257 mL 9.6287 mL 19.2574 mL
    5 mM 0.3851 mL 1.9257 mL 3.8515 mL
    10 mM 0.1926 mL 0.9629 mL 1.9257 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Concentration
    ×
    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

    ×
    体積 （開始）

    V1

    =
    濃度 （終了）

    C2

    ×
    体積 （終了）

    V2

    体内:

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  50% PEG300    50% Saline

      Solubility: 2 mg/mL (3.85 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    純度とドキュメンテーション

    純度: 99.58%

    COA (246 KB) HNMR (175 KB) LCMS (441 KB)

    取扱説明書 (2659 KB)
    参考文献
    細胞実験
    [1]

    For proliferation assays, GIST 882 and TT cells are grown in RPMI medium containing L-glutamine, and MDA-MB-231, HepG2 and A375 cells in DMEM always containing 10% hiFBS. Cells are trypsinized, plated at 5×104 cells/well in 96-well plates in complete media containing 10% FBS and grown overnight at 37°C. The next day, vehicle or regorafenib serially diluted in complete growth media to between 10 μM and 5 nM final concentrations, and 0.2% DMSO, is added and incubation is continued for 96 hr. Cell proliferation is quantified using CellTitre-GloTM.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    動物実験
    [1]

    Female athymic NCr nu/nu mice, kept in accordance with Federal guidelines, are subcutaneously inoculated with 5×106 Colo-205 or MDA-MB-231 cells or implanted with 1 mm3 786-O tumor fragments. When tumors reach a volume of 100 mm3, regorafenib or vehicle control is administered orally qd×21 in the 786-O model, and qd×9 in the Colo-205 and MDA-MB-231 models, respectively, at doses of 100, 30, 10, and 3 mg/kg. Paclitaxel is administered intravenously at 10 mg/kg in ethanol/Cremophor EL®/saline (12.5%/12.5%/75%) every 2 days×5. Tumor size (volume) is estimated twice weekly (l×w2)/2, and the percentage of tumor growth inhibition (TGI) is obtained from terminal tumor weights (1-T/C×100). Mice are weighed every other day starting from the first day of treatment. The general health status of the mice is monitored daily.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9257 mL 9.6287 mL 19.2574 mL 48.1436 mL
    5 mM 0.3851 mL 1.9257 mL 3.8515 mL 9.6287 mL
    10 mM 0.1926 mL 0.9629 mL 1.9257 mL 4.8144 mL
    15 mM 0.1284 mL 0.6419 mL 1.2838 mL 3.2096 mL
    20 mM 0.0963 mL 0.4814 mL 0.9629 mL 2.4072 mL
    25 mM 0.0770 mL 0.3851 mL 0.7703 mL 1.9257 mL
    30 mM 0.0642 mL 0.3210 mL 0.6419 mL 1.6048 mL
    40 mM 0.0481 mL 0.2407 mL 0.4814 mL 1.2036 mL
    50 mM 0.0385 mL 0.1926 mL 0.3851 mL 0.9629 mL
    60 mM 0.0321 mL 0.1605 mL 0.3210 mL 0.8024 mL
    80 mM 0.0241 mL 0.1204 mL 0.2407 mL 0.6018 mL
    100 mM 0.0193 mL 0.0963 mL 0.1926 mL 0.4814 mL
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    Regorafenib Hydrochloride Related Classifications

    • Molarity Calculator

    • Dilution Calculator

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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    質量   濃度   体積   分子量 *
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    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    Help & FAQs
    • 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:

    Regorafenib835621-07-3BAY 73-4506VEGFRAutophagyPDGFRRafRETVascular endothelial growth factor receptorPlatelet-derived growth factor receptorRaf kinasesInhibitorinhibitorinhibit

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    製品番号:
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