Cobimetinib (GDC-0973, RG7420)

製品コードS8041 別名：XL518

Cobimetinib (GDC-0973, RG7420)化学構造

分子量(MW)：531.31

Cobimetinib (GDC-0973, RG7420) is a potent and highly selective MEK1 inhibitor with IC50 of 4.2 nM, showing more than 100-fold selectively for MEK1 over MEK2 and showed no significant inhibition when tested against a panel of more than 100 of serine-threonine and tyrosine kinases. Phase 3.

サイズ 価格(税別)  
JPY 32702.00
JPY 99102.00
JPY 165502.00
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バルク問合せ

文献中Selleckの製品使用例(15)

カスタマーフィードバック(3)

  • Three types of selective inhibitors of MAPK signaling produce expected differential kinase inhibition and activation responses in HCT116 colorectal cancer cells. HCT116 cells were treated with 250 nM of GDC-0973, GDC-0623, SCH772984 or DMSO for 1, 4, or 24 h. In the washout samples, cells were drug treated for 24 h, then changed into fresh media and harvested after 0.5 or 2 h. Lysates were used for Western blots of total and phosphorylated MEK, ERK, and RSK; blotting for COX IV was used as the loading control.

    Mol Cell Proteomics, 2017, 16(2):265-277. Cobimetinib (GDC-0973, RG7420) purchased from Selleck.

  • Western blots showing protein changes of p21, p53, cyclin D1, and cyclin E in HCT116 cells after treatment with 1 μM cobimetinib over different timespans.

    Cell Physiol Biochem, 2018, 47(2):680-693. Cobimetinib (GDC-0973, RG7420) purchased from Selleck.

  • Human-washed platelet aggregation was performed by optical aggregometry following stimulation with U46619 (0.25μM) in the presence or absence of LPS from E. coli O111:B4 (1μg/mL) after 3 min of incubation with Cobimetinib (100μM) before activation with U46619 (0.25μM) (B).

    PLoS One, 2017, 12(11):e0186981. Cobimetinib (GDC-0973, RG7420) purchased from Selleck.

製品安全説明書

MEK阻害剤の選択性比較

生物活性

製品説明 Cobimetinib (GDC-0973, RG7420) is a potent and highly selective MEK1 inhibitor with IC50 of 4.2 nM, showing more than 100-fold selectively for MEK1 over MEK2 and showed no significant inhibition when tested against a panel of more than 100 of serine-threonine and tyrosine kinases. Phase 3.
ターゲット
MEK1 [1]
(Cell-free assay)
4.2 nM
体外試験

Cobimetinib shows strong activity on cell growth inhibtion in a broad panel of tumor types, particularly in BRAF or KRAS mutant cancer cell lines. In combination with GDC-0941, GDC-0973 results in reduced viability, pathway inhibition, and increased apoptosis in 888MEL and A2058 cells. [1] Coadministration of GDC-0973 and vemurafenib significantly increases decreased levels of GLUT-1 on the cellular membrane across all BRAFV600E lines. [2]
細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MDA-MB-231T cells MULGeY5kfGmxbjDhd5NigQ>? MlzXNUBp MXrJcohq[mm2aX;uJI9nKE2HSz3t[YRq[XSnZDDFVmshXDJyMj;ZNlA1KHCqb4PwbI9zgWyjdHnvckBqdiCqdX3hckBOTEFvTVKtNlMyXCClZXzsd{Bi\nSncjCxJIhzKGK7IHntcZVvd2Kub4T0bY5o97zOIFnDOVA:OC5{IH7N NXzxelVsOjR7MEC0PFY>
human COLO205 cells M2f3XWZ2dmO2aX;uJIF{e2G7 NEC4e4NKdmirYnn0bY9vKG:oIFKtdoFnKFZ4MEDFJI12fGGwdDDpckBpfW2jbjDDU2xQOjB3IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kBGWktzL1XST|IheGixc4Doc5J6dGG2aX;uMEBKSzVyPUGuPEBvVQ>? M1PnO|IzOzF3M{Oy
human COLO205 cells NVTNRW5tWHKxbHnm[ZJifGmxbjDhd5NigQ>? MnXQRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCFT1zPNlA2KGOnbHzzJIV5eHKnc4PpcochSi2{YX[gWlYxOEVibYX0ZY51NCCLQ{WwQVghdk1? NXTMeHhoOjJ|MUWzN|I>

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アッセイ
Methods Test Index PMID
Western blot
pERK / ERK / MCL-1 / p-MCL1 / BIM / cleaved PARP; 

PubMed: 27765849     


RKO cells were treated with increasing doses of cobimetinib for 48 h and protein expression, including BIM isoforms [extra long (EL), long (L) and short (S)] and PARP cleavage (CL), were analyzed by immunboblotting. 

p-c-RAF / c-RAF / p-MEK / MEK; 

PubMed: 26384788     


Effect of cobimetinib on MAPK cascade pathway. Changes in activation status of RAF, MEK and ERK were evaluated in three NB cell lines after treatment with cobimetinib (1 μM) or DMSO for four hours. Cell lysates were made with lysis buffer containing prote䲧疝Ỵ疞㧀疜膉痘 瘿⟸෕ᾰƌ෕Ð 㺣痖帉痖Ѐ瑖堘𢡄빢᎒෕Ð鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ戤瘯Ɖ�෋䐺痖暼瘿�෋ᾰƌ �෋Ð㺣痖�෋

27765849 26384788
Growth inhibition assay
Cell viability ; 

PubMed: 28098866     


MEL-XY3 cells were treated with different concentrations of GDC-0973 (0–10 µM) for 72 h and viability was determined using MTT assay. 

28098866
体内試験 In mice bearing BRAFV600E and KRAS mutant tumors, Cobimetinib (10 mg/kg, p.o.) produces antitumor efficacy, and the combination of GDC-0973 and GDC-0941 show improved efficacy. [1] In mice bearing drug-resistant A375 xenografts, combination of GDC-0973 and GDC-0941 induces decreased levels of hexokinase II, c-RAF, Ksr and p-MEK protein. [2]

お薦めの試験操作（参考用のみ）

動物試験：

[1]
+ 展開
  • 動物モデル： Molm-13, Molm-16, MX-1, DLD-1, HCT-116, LoVo, FaDu, 537MEL, A2058, A2058-X1, A375, A375.X1, A427, A549, Calu-6, EBC-1, NCI-H441, NCI-H2122, NCI-H460, NCI-H520.X1, SKOV-3, KP4-X1.1, MiaPaCa-2, 22Rv1, DU-145.X1,S, NCI-H69 xenograft tumors in mice
  • 製剤： --
  • 投薬量： 10 mg/kg
  • 投与方法： p.o.
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 100 mg/mL (188.21 mM)
Ethanol 47 mg/mL warmed (88.46 mM)
Water Insoluble
体内 左から（NMPから）右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
5% DMSO+30% PEG 300+5% Tween 80+ddH2O
混合させたのち直ちに使用することを推奨します。 		5mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 531.31
化学式

C21H21F3IN3O2
CAS No. 934660-93-2
保管 粉
in solvent
別名 XL518

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA（製品ページで利用可能な）。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます：

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます：C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA（オンラインで利用できる）で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください：

総分子量：g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03732703 Not yet recruiting Relapsed Refractory Multiple Myeloma Multiple Myeloma Research Consortium|AbbVie|Celgene Corporation|Eli Lilly and Company|Genentech Inc.|Janssen LP|Takeda March 15 2019 Phase 1|Phase 2
NCT03732703 Not yet recruiting Relapsed Refractory Multiple Myeloma Multiple Myeloma Research Consortium|AbbVie|Celgene Corporation|Eli Lilly and Company|Genentech Inc.|Janssen LP|Takeda March 15 2019 Phase 1|Phase 2
NCT03625141 Recruiting Metastatic Melanoma Hoffmann-La Roche December 13 2018 Phase 2
NCT03625141 Recruiting Metastatic Melanoma Hoffmann-La Roche December 13 2018 Phase 2
NCT03695380 Recruiting OVARIAN CANCER Hoffmann-La Roche November 2 2018 Phase 1
NCT03695380 Recruiting OVARIAN CANCER Hoffmann-La Roche November 2 2018 Phase 1

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

よくある質問（FAQ）

  • 質問1：

    How to reconstitute the inhibitor for in vivo studies?

  • 回答：

    S8041 can be dissolved in 5% DMSO/30% PEG 300/5% Tween 80/ddH2O at 5 mg/ml clearly and it is ok for both oral gavage and injection.

selleck catalog

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID