Entrectinib (Rxdx-101)

製品コードS7998 バッチS799801

化学情報

	Synonyms	RXDX-101, NMS-E628	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₃₁H₃₄F₂N₆O₂
	分子量	560.64	CAS No.	1108743-60-7
Solubility (25°C)*	体外	DMSO	100 mg/mL (178.36 mM)
		Ethanol	100 mg/mL (178.36 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	Entrectinib is an orally bioavailable pan-TrkA/B/C, ROS1 and ALK inhibitor with IC50 ranging between 0.1 and 1.7 nM. Entrectinib (RXDX-101) induces autophagy. Phase 2.
in vitro	Entrectinib selectively blocks proliferation of ALK-dependent cell lines and potently inhibits ALK‐dependent signaling. This compound also highly inhibits cell growth of the NSCLC cell line NCI‐H2228 bearing the EML4-ALK rearrangement.
in vivo	In mice bearing Karpas-299 and SR-786 xenografts, Entrectinib (p.o.) induces complete tumor regression. In NPM-ALK transgenic mice, this compound induces complete regression of tumor masses observed in the thymus and in lymph nodes. In the NB xenograft model, this compound cotreatment enhanced the efficacy of conventional chemotherapy.

製品説明

Entrectinib is an orally bioavailable pan-TrkA/B/C, ROS1 and ALK inhibitor with IC50 ranging between 0.1 and 1.7 nM. Entrectinib (RXDX-101) induces autophagy. Phase 2.

in vitro

Entrectinib selectively blocks proliferation of ALK-dependent cell lines and potently inhibits ALK‐dependent signaling. This compound also highly inhibits cell growth of the NSCLC cell line NCI‐H2228 bearing the EML4-ALK rearrangement.

in vivo

In mice bearing Karpas-299 and SR-786 xenografts, Entrectinib (p.o.) induces complete tumor regression. In NPM-ALK transgenic mice, this compound induces complete regression of tumor masses observed in the thymus and in lymph nodes.

In the NB xenograft model, this compound cotreatment enhanced the efficacy of conventional chemotherapy.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	CUTO28 cells
	濃度	12 nM
	反応時間
	実験の流れ	Cells were treated with different concentrations of entrectinib and proliferation was evaluated.
動物実験	動物モデル	Female NSG mice
	投薬量	50 mg/kg
	投与方法

参考

https://pubmed.ncbi.nlm.nih.gov/26457764/
http://mct.aacrjournals.org/content/8/12_Supplement/A244.short
http://cancerres.aacrjournals.org/content/75/15_Supplement/5390

https://pubmed.ncbi.nlm.nih.gov/36101520/
https://pubmed.ncbi.nlm.nih.gov/33229458/

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カスタマーフィードバック

: Data from [Data independently produced by , , Clin Cancer Res, 2018, 24(10):2357-2369]

: Data from [Data independently produced by , , Clin Cancer Res, 2018, doi: 10.1158/1078-0432.CCR-17-1623]

: Data from [Data independently produced by , , Cancer Med, 2017, 6(12):2972-2983]

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：

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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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