TAK-733

製品コードS2617 バッチS261701

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₇H₁₅F₂IN₄O₄
	分子量	504.23	CAS No.	1035555-63-5
Solubility (25°C)*	体外	DMSO	101 mg/mL (200.3 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <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	TAK-733 is a potent and selective MEK allosteric site inhibitor for MEK1 with IC50 of 3.2 nM, inactive to Abl1, AKT3, c-RAF, CamK1, CDK2, c-Met, etc. Phase 1.
in vitro	TAK-733 is highly potent and selective MEK allosteric site inhibitor with IC50 of 3.2 nM. This compound shows potent enzymatic and cell activity with an EC50 of 1.9 nM against ERK phosphorylation in cells. ^[1]
in vivo	TAK-733 demonstrates broad antitumor activity in mouse xenograft models of human cancer including models of melanoma, colorectal, NSCLC, pancreatic and breast cancer. This compound is well tolerated with pharmacokinetics and pharmacodynamics that support once-daily oral dosing in humans. ^[1] It shows maximally efficacious doses at once daily orally doses of 10 mg/kg. ^[2]

プロトコル(参考用のみ)

動物実験	動物モデル	Human solid tumor xenograft models including NSCLC (NCI H23 [KRAS and LKB1 mutations]), CRC (SW620 [KRAS, APC, p53 mutations]) Pancreatic cancer (Panc 1 and Capan 1 [KRAS mutations] and BxPC-3 [No MAPK mutations]) models in immunocompromised mice.
	投薬量	10 mg/kg
	投与方法	Orally administrated once daily for 21 days

参考

https://pubmed.ncbi.nlm.nih.gov/21310613/
http://cancerres.aacrjournals.org/cgi/content/short/72/8_MeetingAbstracts/3739

カスタマーフィードバック

: Data independently produced by , , Dr.Wang from Southern Medical Hospital

: , , Jonas Nilsson, PhD from University of Gothenburg

: , , Dr. Zhang of Tianjin Medical University

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：

Salmonella effector SopB reorganizes cytoskeletal vimentin to maintain replication vacuoles for efficient infection [ Nat Commun, 2023, 14(1):478]	PubMed: 36717589
Combination of drug therapies and radiation against stem cell-enriched glioblastoma-derived spheres. [ mediaTUM, 2023, ]	PubMed: None
Strategies to inhibit FGFR4 V550L-driven rhabdomyosarcoma [ Br J Cancer, 2022, 10.1038/s41416-022-01973-6]	PubMed: 36097178
Combining HDAC and MEK Inhibitors with Radiation against Glioblastoma-Derived Spheres [ Cells, 2022, 11(5)775]	PubMed: 35269397
Comprehensive drug response profiling and pan-omic analysis identified therapeutic candidates and prognostic biomarkers for Asian cholangiocarcinoma [ iScience, 2022, 25(10):105182]	PubMed: 36248745
Identification of New Vulnerabilities in Conjunctival Melanoma Using Image-Based High Content Drug Screening [ Cancers (Basel), 2022, 14(6)1575]	PubMed: 35326726
Identification and Characterization of a Novel Dual Inhibitor of Indoleamine 2,3-dioxygenase 1 and Tryptophan 2,3-dioxygenase [ Int J Tryptophan Res, 2022, 15:11786469221138456]	PubMed: 36467776
CAGE-prox: A Unified Approach for Time-Resolved Protein Activation in Living Systems [ Curr Protoc, 2021, 1(6):e180]	PubMed: 34165886
Time-resolved protein activation by proximal decaging in living systems [Wang J, et al. Nature, 2019, 569(7757):509-513]	PubMed: 31068699
[ Mol Cancer, 2019, ]	PubMed: 31747941

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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