Entrectinib

製品コードS7998 バッチS799804

印刷

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

25 mg/mL (44.59 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	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. ^[2]
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. ^[2] In the NB xenograft model, this compound cotreatment enhanced the efficacy of conventional chemotherapy. ^[3]

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. ^[2]

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. ^[2]

In the NB xenograft model, this compound cotreatment enhanced the efficacy of conventional chemotherapy. ^[3]

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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Development of PROTACs for targeted degradation of oncogenic TRK fusions [ bioRxiv, 2025, 2025.06.18.660465]	PubMed: 40666929
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Pharmacological inhibition of PDGF-C/neuropilin-1 interaction: A novel strategy to reduce melanoma metastatic potential [ Biomed Pharmacother, 2024, 176:116766]	PubMed: 38788599
Acquired NF2 mutation confers resistance to TRK inhibition in an ex vivo LMNA::NTRK1-rearranged soft-tissue sarcoma cell model [ J Pathol, 2024, 263(2):257-269]	PubMed: 38613194
Acquired NF2 mutation confers resistance to TRK inhibition in an ex vivo LMNA::NTRK1-rearranged soft-tissue sarcoma cell model [ J Pathol, 2024, 10.1002/path.6282]	PubMed: 38613194
LTK mutations responsible for resistance to lorlatinib in non-small cell lung cancer harboring CLIP1-LTK fusion [ Commun Biol, 2024, 7(1):412]	PubMed: 38575808
Patient-derived rhabdomyosarcoma cells recapitulate the genetic and transcriptomic landscapes of primary tumors [ iScience, 2024, 27(10):110862]	PubMed: 39319271

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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