Cobimetinib (GDC-0973)

製品コードS8041 バッチS804103

印刷

化学情報

Synonyms

RG7420,XL518

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₁H₂₁F₃IN₃O₂

分子量

531.31

CAS No.

934660-93-2

Solubility (25°C)*

体外

DMSO

100 mg/mL (188.21 mM)

Ethanol (warmed with 50ºC water bath)

50 mg/mL (94.1 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

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. Cobimetinib induces apoptosis. Phase 3.
in vitro	Cobimetinib (GDC-0973) 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, this compound results in reduced viability, pathway inhibition, and increased apoptosis in 888MEL and A2058 cells. ^[1]
in vivo	In mice bearing BRAFV600E and KRAS mutant tumors, Cobimetinib (GDC-0973) (10 mg/kg, p.o.) produces antitumor efficacy, and the combination of it and GDC-0941 show improved efficacy. ^[1] In mice bearing drug-resistant A375 xenografts, this compound and GDC-0941 induces decreased levels of hexokinase II, c-RAF, Ksr and p-MEK protein. ^[2]

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. Cobimetinib induces apoptosis. Phase 3.

in vitro

Cobimetinib (GDC-0973) 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, this compound results in reduced viability, pathway inhibition, and increased apoptosis in 888MEL and A2058 cells. ^[1]

in vivo

In mice bearing BRAFV600E and KRAS mutant tumors, Cobimetinib (GDC-0973) (10 mg/kg, p.o.) produces antitumor efficacy, and the combination of it and GDC-0941 show improved efficacy. ^[1]

In mice bearing drug-resistant A375 xenografts, this compound and GDC-0941 induces decreased levels of hexokinase II, c-RAF, Ksr and p-MEK protein. ^[2]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	H2122 cells
	濃度	4.2 nM
	反応時間
	実験の流れ	Cells were treated with different concentrations of Cobimetinib (GDC-0973, MEKi) either alone or with PI3K inhibitor (GDC-0941) and assayed for cell death using a Nucleasomal ELISA assay.
動物実験	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
	投薬量	10 mg/kg
	投与方法	p.o.

参考

https://pubmed.ncbi.nlm.nih.gov/22084396/
https://pubmed.ncbi.nlm.nih.gov/22651703/

カスタマーフィードバック

: Data from [Data independently produced by , , Mol Cell Proteomics, 2017, 16(2):265-277]

: Data from [Data independently produced by , , Cell Physiol Biochem, 2018, 47(2):680-693]

: Data from [Data independently produced by , , PLoS One, 2017, 12(11):e0186981]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Restoration of LAT activity improves CAR T cell sensitivity and persistence in response to antigen-low acute lymphoblastic leukemia [ Cancer Cell, 2025, 43(3):482-502.e9]	PubMed: 40068599
Tumor site influences efficacy of MEKi and immunotherapy combinations in pre-clinical model of cholangiocarcinoma [ Hepatology, 2025, 10.1097/HEP.0000000000001439]	PubMed: 40590857
RIT1 Drives Oncogenic Transformation and is an Actionable Target in Lung Adenocarcinoma [ Cancer Res, 2025, 10.1158/0008-5472.CAN-24-3819]	PubMed: 40644578
Separase Inhibition Enhances Gefitinib Sensitivity of Lung Cancer via PTBP1/TAK1/RIPK1-Mediated PANoptosis [ MedComm (2020), 2025, 6(11):e70432]	PubMed: 41122447
Basroparib overcomes acquired resistance to MEK inhibitors by inhibiting Wnt-mediated cancer stemness in KRAS-mutated colorectal cancer [ Biochem Pharmacol, 2025, 235:116842]	PubMed: 40024348
Discovery of Novel RASGRF2 Fusions as a Therapeutic Target in Lung Adenocarcinoma of Never or Light Smokers [ Cancer Sci, 2025, 116(10):2868-2881]	PubMed: 40734624
JAK2 Inhibition Augments the Anti-Proliferation Effects by AKT and MEK Inhibition in Triple-Negative Breast Cancer Cells [ Int J Mol Sci, 2025, 26(13)6139]	PubMed: 40649917
Dihydrotanshinone I enhanced BRAF mutant melanoma treatment efficacy by inhibiting the STAT3/SOX2 signaling pathway [ Front Oncol, 2025, 15:1429018]	PubMed: 39944829
Tumour-selective activity of RAS-GTP inhibition in pancreatic cancer [ Nature, 2024, 629(8013):927-936]	PubMed: 38588697
MEK inhibition prevents CAR-T cell exhaustion and differentiation via downregulation of c-Fos and JunB [ Signal Transduct Target Ther, 2024, 9(1):293]	PubMed: 39438476

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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