Selective JAK3 inhibitor 1

製品コードS8684 バッチS868401

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₁₉H₁₈N₄O₃
	分子量	350.37	CAS No.	1443235-95-7
Solubility (25°C)*	体外	DMSO	70 mg/mL (199.78 mM)
		Ethanol	9 mg/mL (25.68 mM)
		Water	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	Selective JAK3 inhibitor 1 is an irreversible JAK3 inhibitor with Ki values of 0.07 nM, 320 nM, 740 nM for JAK3, JAK1 and JAK2 respectively. It is also selective over the other kinases possessing a cysteine in the same region as JAK3, such as BMX, EGFR, ITK, and BTK.
in vitro	Selective JAK3 inhibitor 1 is a potent inhibitor of JAK3 (IC50 = 0.15 nM) was 4300-fold selective for JAK3 over JAK1 in enzyme assays, 67-fold [interleukin (IL)-2 versus IL-6] or 140-fold [IL-2 versus erythropoietin or granulocyte-macrophage colony-stimulating factor (GMCSF)] selective in cellular reporter assays and >35-fold selective in human peripheral blood mononuclear cell assays (IL-7 versus IL-6 or GMCSF). The compound blocks cytokine signaling through JAK3, but not through other JAK family enzymes. It inhibits IL-7, IL-15, and IL-2 signaling in T cells, but does not inhibit any other cytokine signaling pathways^[1].
in vivo	Selective JAK3 inhibitor 1 has a partial effect on reversing inflammation and bone loss in the rat CIA model when administered therapeutically during the inflammatory phase of the model at doses that meet or exceed the exposure required for complete inhibition of the phenotype when dosed prophylactically. It inhibits leukocyte proliferation, but not erythrocyte proliferation in rats. Selective JAK3 inhibitor 1 could fully inhibit the development of inflammation^[1].

プロトコル(参考用のみ)

参考

[1] Elwood F, et al. J Pharmacol Exp Ther. 2017, 361(2):229-244.

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：

EBV-positive pyothorax-associated lymphoma expresses CXCL9 and CXCL10 chemokines that attract cytotoxic lymphocytes via CXCR3 [ Cancer Sci, 2023, 114(6):2622-2633]	PubMed: 36898851

EBV-positive pyothorax-associated lymphoma expresses CXCL9 and CXCL10 chemokines that attract cytotoxic lymphocytes via CXCR3 [ Cancer Sci, 2023, 114(6):2622-2633]

PubMed: 36898851

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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