SGC 0946

製品コードS7079 バッチS707902

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

C₂₈H₄₀BrN₇O₄

分子量

618.57

CAS No.

1561178-17-3

Solubility (25°C)*

体外

DMSO

100 mg/mL (161.66 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	SGC 0946 is a highly potent and selective DOT1L methyltransferase inhibitor with IC50 of 0.3 nM in a cell-free assay, is inactive against a panel of 12 PMTs and DNMT1.
in vitro	SGC 0946 is over 100-fold selective for other histone methyltransferases/HMTs. This compound potently reduces H3K79 dimethylation with IC50 of 2.6 nM in A431 cells, and 8.8 nM in MCF10A cells, which potently and selectively kills cells containing an MLL translocation. It is much more potent than its close analog EPZ004777, and serves as an excellent chemical probe for investigating DOT1L and further development of DOT1L inhibitors for cancer therapy. ^[1]
in vivo	SGC0946, a highly potent and selective DOT1L methyltransferase inhibitor, resulted in significant inhibition of tumor progression in the ovarian orthotopic xenograft mice model.
特徴	Cell-active DOT1L-selective chemical probe.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Molm13 cell
	濃度	1 µM
	反応時間	4 days
	実験の流れ	Cells were treated with indicated concentration of this compound for 4 days.
動物実験	動物モデル	Female NOD-SCID mice
	投薬量	10 mg/kg
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/23250418/
https://pubmed.ncbi.nlm.nih.gov/28114995/

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：

Reconstitution of pluripotency from mouse fibroblast through Sall4 overexpression [ Nat Commun, 2024, 15(1):10787]	PubMed: 39737935
Transplantation of derivative retinal organoids from chemically induced pluripotent stem cells restored visual function [ NPJ Regen Med, 2024, 9(1):42]	PubMed: 39730340
Micronucleus is not a potent inducer of the cGAS/STING pathway [ Life Sci Alliance, 2024, 7(4)e202302424]	PubMed: 38307626
Generation and characterization of giant panda induced pluripotent stem cells [ Sci Adv, 2024, 10(38):eadn7724]	PubMed: 39303041
DOT1L stimulates MYC/Mondo transcription factor activity by promoting its degradation cycle on chromatin [ bioRxiv, 2024, 2024.02.06.579191]	PubMed: 38370658
Histone H3K79 methylation by DOT1L promotes Aurora B localization at centromeres in mitosis [ Cell Rep, 2023, 42(8):112885]	PubMed: 37494186
Transcriptome-based chemical screens identify CDK8 as a common barrier in multiple cell reprogramming systems [ Cell Rep, 2023, 42(6):112566]	PubMed: 37235474
The human leukemic oncogene MLL-AF4 promotes hyperplastic growth of hematopoietic tissues in Drosophila larvae [ iScience, 2023, 26(10):107726]	PubMed: 37720104
The human leukemic oncogene MLL-AF4 promotes hyperplastic growth of hematopoietic tissues in Drosophila larvae [ iScience, 2023, 26(10):107726]	PubMed: 37720104
Derivation of totipotent-like stem cells with blastocyst-like structure forming potential [ Cell Res, 2022, 10.1038/s41422-022-00668-0]	PubMed: 35508506

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。