Home > MEK & > Cobimetinib

Cobimetinib

XL518,GDC-0973,RG7420,XL 518,XL-518,RG 7420,RG-7420

Cobimetinib是MEK1/2高选择性抑制剂。

目录号
EY0598
EY0598
EY0598
纯度
99.65%
99.65%
99.65%
规格
2 mg
5 mg
10 mg
原价
390
860
1100
售价
390
860
1100
库存
现货
现货
现货
订购
订购
订购
订购
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  • 生物活性

    Cobimetinib (GDC-0973, RG7420) is a potent and highly selective MEK1 inhibitor with IC50 of 4.2 nM. Phase 3.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

    10 mg/kgp.o.

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] Hoeflich KP, et al. Cancer Res. 2012, 72(1), 210-219.
    [2] Choo EF, et al. PK-PD modeling of combination efficacy effect from administration of the MEK inhibitor GDC-0973 and PI3K inhibitor GDC-0941 in A2058 xenografts. Cancer Chemother Pharmacol. 2013 Jan;71(1):133-43.
    [3] Wong H, et al. Bridging the gap between preclinical and clinical studies using pharmacokinetic-pharmacodynamic modeling: an analysis of GDC-0973, a MEK inhibitor. Clin Cancer Res. 2012 Jun 1;18(11):3090-9.

    分子式
    C21H21F3IN3O2    		 分子量
    531.31    		 CAS号
    934660-93-2    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    100 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    45 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT02537600 Malignant Melanoma Drug: Cobimetinib + Vemurafenib combination treatment Center Eugene Marquis Phase 2 2015-12-01 2016-12-02
    NCT02649972 Histiocytic Disorders Drug: Cobimetinib Memorial Sloan Kettering Cancer Center|Genentech, Inc. Phase 2 2016-01-01 2016-09-14
    NCT02427893 Melanoma Drug: Cobimetinib|Drug: Vemurafenib Sidney Kimmel Comprehensive Cancer Center|Genentech, Inc. Phase 3 2015-08-01 2016-11-14
    NCT02639546 Solid or Brain Tumor With Evidence of RAS/RAF/MEK/ERK Activation Drug: Cobimetinib Hoffmann-La Roche Phase 1|Phase 2 2016-05-31 2017-03-16
    NCT01929876 Healthy Participants Drug: Cobimetinib|Drug: Itraconazole Genentech, Inc. Phase 1 2013-07-01 2016-06-22
    NCT01277718 Healthy Volunteer Drug: Cobimetinib|Drug: Rabeprazole Genentech, Inc. Phase 1 2011-01-01 2016-05-27
    NCT01986166 Neoplasms Drug: Cobimetinib|Drug: MEHD7945A Genentech, Inc. Phase 1 2013-11-01 2016-07-14
    NCT01271803 Malignant Melanoma Drug: Cobimetinib|Drug: vemurafenib Hoffmann-La Roche Phase 1 2011-02-01 2016-05-11
    NCT01988896 Solid Tumors Drug: Atezolizumab|Drug: Cobimetinib Hoffmann-La Roche Phase 1 2013-12-01 2017-03-02
    NCT03005639 Stage IIIB-C Melanoma Drug: Vemurafenib and Cobimetinib Inova Health Care Services|Genentech, Inc. Phase 2 2016-12-01 2016-12-22
    NCT02230306 Active Melanoma Brain Metastases Drug: Cobimetinib|Drug: Vemurafenib Melissa Burgess, MD|Genentech, Inc.|University of Pittsburgh Phase 2 2015-02-01 2016-04-04
    NCT02036086 Melanoma Drug: Vemurafenib|Drug: Cobimetinib Sunnybrook Health Sciences Centre Phase 2 2015-08-01 2016-10-14
    NCT01495988 Melanoma|Metastatic Melanoma Drug: Vemurafenib|Drug: Bevacizumab|Drug: Cobimetinib Melanoma Research Foundation Breakthrough Consortium|Genentech, Inc. Phase 2 2013-08-01 2016-09-12
    NCT01689519 Malignant Melanoma Drug: Placebo|Drug: Vemurafenib|Drug: Cobimetinib Hoffmann-La Roche Phase 3 2013-01-01 2016-07-29
    NCT00467779 Solid Tumor Drug: cobimetinib|Drug: dextromethorphan|Drug: midazolam Genentech, Inc. Phase 1 2007-05-01 2016-07-25
    NCT02303951 Malignant Melanoma Drug: Vemurafenib + cobimetinib University Hospital Tuebingen Phase 2 2015-01-01 2016-05-11
    NCT02968303 Melanoma, Malignant, of Soft Parts Drug: Vemurafenib and Cobimetinib Radboud University|The Netherlands Cancer Institute|Isala Phase 2 2016-12-01 2016-11-15
    NCT01562275 Neoplasms Drug: Ipatasertib|Drug: Cobimetinib Genentech, Inc. Phase 1 2012-04-01 2016-02-25
    NCT00996892 Solid Tumors Drug: Cobimetinib|Drug: Pictilisib Genentech, Inc. Phase 1 2009-11-01 2016-11-04
    NCT01249118 Healthy Volunteers Drug: GDC-0973 IV Infusion|Drug: GDC-0973 Oral Capsules Genentech, Inc. Phase 1 2010-11-01 2016-12-12

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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