CEP-40783 (RXDX-106)

製品コードS8570 バッチS857001

印刷

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

C₃₁H₂₆F₂N₄O₆

分子量

588.56

CAS No.

1437321-24-8

Solubility (25°C)*

体外

DMSO

10 mg/mL (16.99 mM)

Ethanol

2 mg/mL (3.39 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	CEP-40783 (RXDX-106) is an orally-available, potent and selective TAM(TYRO3, AXL, MER)/Met (c-Met) inhibitor displaying low nanomolar biochemical activity and slow (T1/2 >120 min) inhibitor off-rate in peptide phosphorylation assays and in vitro kinase binding assays, respectively.
in vitro	RXDX-106 inhibits TAM and c-MET phosphorylation in vitro. This inhibition of TAM and c-MET activation in vitro is accompanied by a decrease in downstream MAPK and PI3K signaling and cell viability^[1]. It completely inhibits cellular proliferation and viability at sub-nanomolar concentrations in TAM-expressing cells^[2].
in vivo	RXDX-106 could inhibit tumors harboring activating TAM gene fusions and affect the TAM-expressing tumor microenvironment to result in a global anti-cancer environment^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	3T3 cells
	濃度	0.25, 1, 2.5, 10, 25, 100, 250 nM
	反応時間	30 min
	実験の流れ	3T3 cells expressing Tyro3, Axl, or Mer are incubated with vehicle alone or RXDX-106 for 30 minutes, and receptor phosphorylation is monitored.
動物実験	動物モデル	SCID Beige mice
	投薬量	30 mg/kg
	投与方法	p.o.

参考

http://cancerres.aacrjournals.org/content/77/13_Supplement/4191
https://ignyta.com/files/Ignyta_EORTC_NCI_AACR_2016_RXDX106_nonIO_FINAL3-b.pdf

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：

Dissecting AXL-mediated bypass resistance and collateral phenotypes by phosphosite perturbations [ UNIVERSITY OF CALIFORNIA, 2023, ]	PubMed: None
Dissecting signaling regulators driving AXL-mediated bypass resistance and associated phenotypes by phosphosite perturbations [ bioRxiv, 2023, 2023.10.20.563266]	PubMed: 37961516
Integrated Proteomics-Based Physical and Functional Mapping of AXL Kinase Signaling Pathways and Inhibitors Define Its Role in Cell Migration [ Mol Cancer Res, 2022, 20(4):542-555]	PubMed: 35022314
Inhibition of Axl Promotes the Therapeutic Effect of Targeted Inhibition of the PI3K/Akt Pathway in NRAS Mutant Melanoma Cells [ J Oncol, 2022, 2022:2946929]	PubMed: 35310910
Cell Type-specific Adaptive Signaling Responses to KRASG12C Inhibition [ Clin Cancer Res, 2021, 27(9):2533-2548]	PubMed: 33619172
Attenuation of apoptotic cell detection triggers thymic regeneration after damage [ Cell Rep, 2021, 37(1):109789]	PubMed: 34610317
Lysyl-tRNA synthetase-expressing colon spheroids induce M2 macrophage polarization to promote metastasis. [ J Clin Invest, 2018, 128(11):5034-5055]	PubMed: 30188867

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。