Alectinib (CH5424802) hydrochloride

製品コードS5232 バッチS523202

印刷

化学情報

Synonyms

AF802, RO5424802, RG-7853

Storage
(From the date of receipt)

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

化学式

C₃₀H₃₄N₄O₂.HCl

分子量

519.08

CAS No.

1256589-74-8

Solubility (25°C)*

体外

DMSO

2 mg/mL (3.85 mM)

Water

Insoluble

Ethanol

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	Alectinib (AF802, CH5424802, RO5424802, RG-7853) is a second generation oral drug that selectively inhibits the activity of anaplastic lymphoma kinase (ALK) tyrosine kinase.
in vitro	Alectinib inhibits ALK with an IC50 value of 1.9 nmol/L and shows higher selectivity for ALK than for a number of other serine/tyrosine kinases. It also inhibits the ALK gatekeeper mutation L1196M with an IC50 of 1.56 nmol/L. Alectinib is effective with PF-02341066-resistant ALK mutations L1196M, F1174L, R1275Q and C1156Y. In the KARPAS-299 (lymphoma), NB-1 (neuroblastoma) and NCI-H2228 (lung cancer) ALK-positive cell lines, alectinib inhibits cell proliferation with IC50 values of 3, 4.5 and 53 nmol/L, respectively^[1].
in vivo	Alectinib dose-dependently inhibits EML4-ALK positive NCI-H2228 xenograft model at doses ranging from 2 to 20 mg/kg p.o., q.d. Significant efficacy is also achieved in the EML4-ALK L1196M-driven tumors^[1]. It has antitumor activity against cancers with ALK gene alterations^[2].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	KB cells
	濃度	0.01-100 μM
	反応時間	72 h
	実験の流れ	---
動物実験	動物モデル	SCID mice inocubated with subcutaneous tumors
	投薬量	60 mg/kg
	投与方法	Oral administration

参考

https://pubmed.ncbi.nlm.nih.gov/26579422/
https://pubmed.ncbi.nlm.nih.gov/24887559/
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5382559/

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：

AXL and SHC1 confer crizotinib resistance in patient-derived xenograft model of ALK-driven lung cancer [ iScience, 2024, 27(9):110846]	PubMed: 39310759
Tyrosine Kinase Inhibitors Target B Lymphocytes [ Biomolecules, 2023, 13(3)438]	PubMed: 36979373
Crizotinib attenuates cancer metastasis by inhibiting TGFβ signaling in non-small cell lung cancer cells [ Exp Mol Med, 2022, 54(8):1225-1235]	PubMed: 35999455
HER3 activation contributes toward the emergence of ALK inhibitor-tolerant cells in ALK-rearranged lung cancer with mesenchymal features [ NPJ Precis Oncol, 2022, 6(1):5]	PubMed: 35042943
Novel human-derived EML4-ALK fusion cell lines identify ribonucleotide reductase RRM2 as a target of activated ALK in NSCLC [ Lung Cancer, 2022, 171:103-114]	PubMed: 35933914
Discovery of a novel ALK/ROS1/FAK inhibitor, APG-2449, in preclinical non-small cell lung cancer and ovarian cancer models [ BMC Cancer, 2022, 22(1):752]	PubMed: 35820889
Downregulation of PD-L1 and HLA-I in non-small cell lung cancer with ALK fusion [ Thorac Cancer, 2022, 10.1111/1759-7714.14372]	PubMed: 35253386
The CLIP1-LTK fusion is an oncogenic driver in non-small-cell lung cancer [ Nature, 2021, 600(7888):319-323]	PubMed: 34819663
Inhibition of c-Jun N-terminal kinase signaling increased apoptosis and prevented the emergence of ALK-TKI-tolerant cells in ALK-rearranged non-small cell lung cancer [ Cancer Lett, 2021, 522:119-128]	PubMed: 34534615
SHP2 inhibition enhances the effects of tyrosine kinase inhibitors in preclinical models of treatment-naïve ALK-, ROS1-, or EGFR-altered non-small-cell lung cancer [ Mol Cancer Ther, 2021, molcanther.0965.2020]	PubMed: 34158345

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。