A-1155463 Dihydrochloride

製品コードS7800 バッチS780002

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

C₃₅H₃₄Cl₂FN₅O₄S₂

分子量

742.71

CAS No.

1235034-55-5(free base)

Solubility (25°C)*

体外

DMSO

100 mg/mL (134.64 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	A-1155463 Dihydrochloride, a highly potent and selective BCL-XL inhibitor, shows picomolar binding affinity to BCL-XL, and >1000-fold weaker binding to BCL-2 and related proteins BCL-W(Ki=19 nM) and MCL-1(Ki>440 nM).
in vitro	A-1155463 Dihydrochloride disrupts BCL-XL-BIM but not BCL-2-BIM complexes in cells. A-1155463 kills BCL-XL-dependent Molt-4 cells (EC50=70 nM) but has no measurable cytotoxicity against BCL-2-dependent RS4;11 cells (EC50>5 mM). A-1155463 induces the hallmarks of apoptosis, as evidenced by the release of cytochrome c from mitochondria, caspase activation, and the accumulation of caspase-dependent sub-G0-G1 DNA content in BCL-XL-dependent H146 cells^[2].
in vivo	Following a single 5 mg/kg IP dose of A-1155463 in nontumor bearing SCID-Beige mice, platelet counts fall dramatically as measured at 6 h postdose and then rebound to normal levels within 72 h. Daily Dosing at 5 mg/kg IP to SCID-Beige mice that had been inoculated with BCL-XL-dependent H146 tumor cells for 14 days causes a statistically significant inhibition of tumor growth (maximum tumor growth inhibition = 44%), which is alleviated upon cessation of dosing^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Colorectal cell lines (ATCC)
	濃度	0-10 μM
	反応時間	72 h
	実験の流れ	Cells are treated with increasing concentration of A-1155463. Cells are assayed for viability after 72 h using the CellTiter-Glo luminescent cell viability assay according to the manufacturer’s protocol. Results are normalized to cells without treatment. EC50 is calculated using the GraphPad Prism software.
動物実験	動物モデル	SCID-Beige Mice
	投薬量	5 mg/kg
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/25313317/
https://pubmed.ncbi.nlm.nih.gov/25787766/
https://www.infona.pl/resource/bwmeta1.element.springer-doi-10_1186-S12943-015-0397-Y

カスタマーフィードバック

: Data from [Data independently produced by , , Oncogenesis, 2018, 7(9):74]

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：

20(S)-protopanaxadiol inhibits proliferation and induces apoptosis of acute myeloid leukemia cells via targeting Bcl-XL and MCL-1 [ Front Pharmacol, 2025, 16:1530270]	PubMed: 40400713
Therapy-induced normal tissue damage promotes breast cancer metastasis [ iScience, 2024, 27(1):108503]	PubMed: 38161426
Mitochondria of T Lymphocytes Promote Anti-Pulmonary Tumor Immune Response [ World J Oncol, 2024, 15(3):472-481]	PubMed: 38751696
Inhibition of NEK2 Promotes Chemosensitivity and Reduces KSHV-positive Primary Effusion Lymphoma Burden [ Cancer Res Commun, 2024, 4(4):1024-1040]	PubMed: 38592451
Clearance of defective muscle stem cells by senolytics restores myogenesis in myotonic dystrophy type 1 [ Nat Commun, 2023, 14(1):4033]	PubMed: 37468473
TRAF4-mediated ubiquitination-dependent activation of JNK/Bcl-xL drives radioresistance [ Cell Death Dis, 2023, 14(2):102]	PubMed: 36765039
Dual Targeting of Apoptotic and Signaling Pathways in T-Lineage Acute Lymphoblastic Leukemia [ Clin Cancer Res, 2023, 29(16):3151-3161]	PubMed: 37363966
Co-targeting BCL-XL and MCL-1 with DT2216 and AZD8055 synergistically inhibit small-cell lung cancer growth without causing on-target toxicities in mice [ Cell Death Discov, 2023, 9(1):1]	PubMed: 36588105
Co-targeting BCL-XL and MCL-1 with DT2216 and AZD8055 synergistically inhibit small-cell lung cancer growth without causing on-target toxicities in mice [ Cell Death Discov, 2023, 9(1):1]	PubMed: 36588105
The centrosomal protein 131 participates in the regulation of mitochondrial apoptosis [ Commun Biol, 2023, 6(1):1271]	PubMed: 38102401

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。