S63845

製品コードS8383 バッチS838304

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

C₃₉H₃₇ClF₄N₆O₆S

分子量

829.26

CAS No.

1799633-27-4

Solubility (25°C)*

体外

DMSO

100 mg/mL (120.58 mM)

Ethanol

100 mg/mL (120.58 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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	5.000mg/ml (6.03mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <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	S63845 is a new, selective MCL-1 inhibitor with the Kd value of 0.19 nM and has no discernible binding to the other BCL-2 members, BCL-2 or BCL-XL.
in vitro	S63845 induces death of cancer cell lines with known reliance on MCL-1, displaying classical hallmarks of apoptosis that are dependent on caspases and BAX/BAK-mediated mitochondrial outer membrane permeabilisation. It has a 6 fold higher affinity for human MCL-1 over mouse MCL-1^[1]. This compound is effective against haematological cancer-derived cell lines in vitro and in vivo and also AML samples, but does not readily kill normal human haematopoietic progenitor cells^[2].
in vivo	In vivo, S63845 shows potent anti-tumour activity with an acceptable safety margin as a single agent in several cancers. This compound is well tolerated by the mice with no significant weight loss observed. Some of solid tumour models shows sensitivity to this compound monotherapy, while many others are only killed when treated with a combination of this compound and inhibitors of oncogenic kinases^[2].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	HeLa cells
	濃度	0.1, 0.3, 1, 3 μM
	反応時間	4 h
	実験の流れ	HeLa cells transduced with Flag–BCL-XL, Flag–BCL-2 or Flag–MCL1 expression constructs are treated for 4 h with increasing concentrations of S63845, before immunopreciptation using anti-FLAG antibody. Immunoprecipitates and total inputs are analysed by immunoblotting for the FLAG-tagged proteins as well as the associated BAK and BAX proteins.
動物実験	動物モデル	C57BL/6 mice
	投薬量	25 mg/kg
	投与方法	i.v.

参考

http://jxym.amegroups.com/article/view/4013
https://pubmed.ncbi.nlm.nih.gov/27760111/

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：

Co-targeting of epigenetic regulators and BCL-XL improves efficacy of immune checkpoint blockade therapy in multiple solid tumors [ Mol Cancer, 2025, 24(1):154]	PubMed: 40442785
Myeloid EGFR deficiency accelerates recovery from AKI via macrophage efferocytosis and neutrophil apoptosis [ Nat Commun, 2025, 16(1):4563]	PubMed: 40379634
Synergistic activity of S63845 and parthenolide to overcome acquired resistance to MEK1/2 inhibitor in melanoma cells: Mechanisms and therapeutic potential [ Biomed Pharmacother, 2025, 188:118183]	PubMed: 40424823
BH3 mimetics augment cytotoxic T cell killing of acute myeloid leukemia via mitochondrial apoptotic mechanism [ Cell Death Discov, 2025, 11(1):120]	PubMed: 40140361
Mitochondrial priming and response to BH3 mimetics in "one-two punch" senogenic-senolytic strategies [ Cell Death Discov, 2025, 11(1):91]	PubMed: 40055336
BDA-366 inhibits extra-nodal natural killer/T-cell lymphoma by inducing mitochondria damage through NF-κB pathway [ Biochem Pharmacol, 2025, S0006-2952(25)00712-9]	PubMed: 41135664
Bcl‑xL‑specific BH3 mimetic A‑1331852 suppresses proliferation of fluorouracil‑resistant colorectal cancer cells by inducing apoptosis [ Oncol Rep, 2025, 53(2)26]	PubMed: 39717947
Senolytic compounds reduce epigenetic age of blood samples in vitro [ NPJ Aging, 2025, 11(1):6]	PubMed: 39905063
Tumor nutrient stress gives rise to a drug tolerant cell state in pancreatic cancer [ bioRxiv, 2025, 2025.09.04.673818]	PubMed: 40964288
Direct Co-Targeting of Bcl-xL and Mcl-1 Exhibits Synergistic Effects in AR-V7-Expressing CRPC Models [ Cancer Res Commun, 2025, 5(8):1396-1408]	PubMed: 40704654

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。