1. PI3K/Akt/mTOR
    Apoptosis
  2. mTOR
    Apoptosis
  3. CC-223

CC-223 

製品番号: HY-16956 純度: 99.43%
取扱説明書

CC-223 is a potent, selective, and orally bioavailable inhibitor of mTOR kinase, with an IC50 value for mTOR kinase of 16 nM. CC-223 inhibits both mTORC1 and mTORC2.

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CC-223 構造式

CC-223 構造式

CAS 番号 : 1228013-30-6

容量 価格(税別) 在庫状況 数量
10 mM * 1 mL in DMSO USD 158 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 144 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 228 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 900 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 1320 在庫あり
Estimated Time of Arrival: December 31
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

カスタマーレビュー

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products

    CC-223 purchased from MCE. Usage Cited in: Oncotarget. 2017 May 10;8(35):58469-58479.

    CC223 blocks mTORC1 and mTORC2 activation in SKOV3 cells. SKOV3 cells are treated with CC223 (100 nM), cells are further cultured for implied time, mTOR-Raptor and mTOR-Rictor assembly is tested by Co-immunoprecipitation assay. Expressions of listed proteins are tested by the Western blotting assay.

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    製品説明

    CC-223 is a potent, selective, and orally bioavailable inhibitor of mTOR kinase, with an IC50 value for mTOR kinase of 16 nM. CC-223 inhibits both mTORC1 and mTORC2.

    IC50 & Target[1]

    mTOR

    16 nM (IC50)

    mTORC1

     

    mTORC2

     

    DNA-PK

    0.84 μM (IC50)

    PI3K-α

    4 μM (IC50)

    体外実験

    CC-223 is a potent, selective, and orally bioavailable inhibitor of mTOR kinase, demonstrating inhibition of mTORC1 (pS6RP and p4EBP1) and mTORC2 [pAKT(S473)] in cellular systems. CC-223 is selective for mTOR kinase with >200-fold selectivity over the related PI3K-α (IC50=4.0 μM). Of the PI3K related kinases tested, CC-223 shows no significant inhibition of ATR or SMG1 and inhibits DNA-PK with an IC50 value of 0.84 μM. When screened in a single-point assay against a commercially available panel of 246 kinases, only three kinases other than mTOR are inhibited >80% at 10 μM by CC-223. Upon follow-up IC50 value determination, only two are inhibited by CC-223 with IC50 values below 1 μM; FLT4 (0.651 μM) and cFMS (0.028 μM). The exquisite kinase selectivity of CC-223 is confirmed upon evaluation in cellular systems using ActivX KiNavtiv profiling. Other than mTOR kinase, no kinase target is identified when HCT 116 or A549 cells are treated for 1 hour with 1 μM CC-223 and assayed for kinase activity. CC-223 shows a concentration-dependent reduction in each marker, with IC50 values of 31±2 nM for pS6RP, 405±47 nM for p4EBP1, and 11±10 nM for pAKT(S473) in western blot analysis. Inhibition of these pathway biomarkers is investigated in additional cell types from a variety of tissue origins. CC-223 inhibits both mTORC1 (S6RP and 4EBP1) and mTORC2 [AKT(S473)] markers across the panel with IC50 ranges of 27 to 184 nM for pS6RP, 120 to 1,050 nM for p4EBP1 and 11 to 150 nM for pAKT(S473) [1].

    体内実験

    The antitumor activity of CC-223 in the PC-3 xenograft model is determined using a number of dosing paradigms. CC-223 significantly inhibits PC-3 tumor growth in a dose- and schedule-dependent manner. Dosing at 10 or 25 mg/kg, once daily, results in 46% (P<0.001) and 87% (P<0.001) reduction in tumor volume, respectively. Similar dose dependency is observed with twice-daily dosing at 5 or 10 mg/kg, corresponding to 65% (P<0.001) and 80% (P<0.001) tumor volume reductions. All dose levels are tolerated in the once-daily and twice-daily dosing studies, with only the 25 mg/kg/d group showing any significant body weight loss. These mice lost approximately 10% of their initial body weight after 3 weeks of dosing[1].

    臨床実験
    分子量

    397.47

    分子式

    C₂₁H₂₇N₅O₃

    CAS 番号

    1228013-30-6

    SMILES

    O=C1CNC2=NC=C(C3=CC=C(C(C)(O)C)N=C3)N=C2N1[[email protected]]4CC[[email protected]](OC)CC4

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : ≥ 27 mg/mL (67.93 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5159 mL 12.5796 mL 25.1591 mL
    5 mM 0.5032 mL 2.5159 mL 5.0318 mL
    10 mM 0.2516 mL 1.2580 mL 2.5159 mL
    *Please refer to the solubility information to select the appropriate solvent.
    参考文献
    キナーゼ実験
    [1]

    Counter screen against 246 protein kinases is outsourced and completed at a fixed CC-223 concentration (10 μM). Follow-up IC50 value determinations for ephrin type-B receptor 3 kinase (EPHB3), colony stimulating factor 1 receptor tyrosine kinase (CSF1R or cFMS), and FMS-related tyrosine kinase 4 (FLT4) are outsourced to Invitrogen[1].

    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。

    細胞実験
    [1]

    For other cell panel proliferation assays, CC-223 (1 nM, 100 nM and 1 μM) is spotted via an acoustic dispenser (EDC ATS-100) into an empty 384-well plate. Cells are diluted to desired densities and added directly to the compound-spotted plates. Cells are allowed to grow for 72 hours. Viability is assessed via Cell Titer-Glo. All data are normalized and represented as a percentage of the DMSO-treated cells. Results are then expressed as GI50 and/or IC50 values[1].

    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]

    Mice[1]
    Female 6- to 8-weeks-old CB17 SCID mice are inoculated s.c. with 2×106 PC-3 cells. When tumors reach approximately 125 mm3, mice are randomized and treated once daily, twice daily, or every 2 days orally with vehicle or various doses of CC-223, at a dose volume of 5 mL/kg. The twice-daily doses are administered with a 10 hours separation between the morning and evening doses. Tumor volumes are determined before the initiation of treatment and are considered as the starting volumes. Tumors are measured twice a week for the duration of the study. The long and short axes of each tumor are measured using a digital caliper in millimeters. The tumor volumes are calculated. The tumor volumes are expressed in cubic millimeters (mm3).

    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

    純度: 99.43%

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    Keywords:

    CC-223CC223CC 223mTORApoptosisMammalian target of RapamycinInhibitorinhibitorinhibit

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    製品名:
    CC-223
    製品番号:
    HY-16956
    数量:
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