LDC4297

製品コードS7992 バッチS799201

印刷

化学情報

Synonyms

LDC044297

Storage
(From the date of receipt)

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

化学式

C₂₃H₂₈N₈O

分子量

432.52

CAS No.

1453834-21-3

Solubility (25°C)*

体外

DMSO

86 mg/mL (198.83 mM)

Ethanol

86 mg/mL (198.83 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。	4.300mg/ml (9.94mM)	Taking the 1 mL working solution as an example, add 50 μL of 86 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 clarify; 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.
Clear solution	5% DMSO 1 95% Corn oil 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。	1.075mg/ml (2.49mM)	Taking the 1 mL working solution as an example, add 50 μL of 21.5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. 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	LDC4297 is a novel CDK7 inhibitor (IC50=0.13±0.06 nM for CDK7 versus IC50s between 10 nM and 10,000 nM for all other analyzed CDKs).
in vitro	LDC4297 inhibits CDK7 in vitro in the nano-picomolar range. The affinity of this compound for CDK7 proves to be extremely high. The replication of HCMV in cultured primary human fibroblasts (HFFs) is inhibited by this chemical in a concentration-dependent manner with a 50% effective concentration (EC50) value of 24.5 ± 1.3 nM. Notably, CDK7 inhibition by this inhibitor is not associated with general cytotoxicity at submicromolar concentrations. In contrast, it induces cytotoxicity in a set of tumor cell lines, i.e., already at extremely low, nanomolar concentrations in specific cases. Anti-HCMV activity of this compound is exerted through a multifaceted mode of action that involves an interference with virus-induced Rb phosphorylation^[1].
in vivo	The PK analyses of LDC4297 performed thus far have also been highly promising. An analysis of the PK parameters in CD1 mice reveals positive characteristics after oral administration, as demonstrated for a single-dose treatment (100 mg/kg of this compound. The half-life (t_1/2z) is determined to be 1.6 h, and a time (Tmax) to a mean peak plasma concentration of 1,297.6 ng/ml is reached 0.5 h after administration, with a continued presence of this chemical's plasma levels for at least 8 h and a bioavailability of 97.7%^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	human fibroblasts
	濃度	0.1 to 50 μM
	反応時間	3 days
	実験の流れ	A trypan blue exclusion assay is performed with cultured cells seeded in 24-well plates and incubated with increasing concentrations of antiviral compounds (range, 0.1 to 50 μM) for the durations indicated. Cell staining is achieved with 0.1% trypan blue for 10 min at room temperature before the percentage of viable cells is determined by microscopic counting.
動物実験	動物モデル	CD-1 mice
	投薬量	100 mg/kg
	投与方法	oral administration

参考

https://pubmed.ncbi.nlm.nih.gov/25624324/

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：

Combined therapy with DR5-targeting antibody-drug conjugate and CDK inhibitors as a strategy for advanced colorectal cancer [ Cell Rep Med, 2025, S2666-3791(25)00231-9]	PubMed: 40449480
Resistance to CDK7 inhibitors directed by acquired mutation of a conserved residue in cancer cells [ EMBO J, 2025, 10.1038/s44318-025-00554-6]	PubMed: 40921851
A deep single cell mass cytometry approach to capture canonical and noncanonical cell cycle states [ bioRxiv, 2025, 2025.07.08.663243]	PubMed: 40672327
CDK7/12/13 inhibition targets an oscillating leukemia stem cell network and synergizes with venetoclax in acute myeloid leukemia [ EMBO Mol Med, 2022, e14990]	PubMed: 35253392
Elevation of effective p53 expression sensitizes wild-type p53 breast cancer cells to CDK7 inhibitor THZ1 [ Cell Commun Signal, 2022, 20(1):96]	PubMed: 36058938
Ubiquitylation of MYC couples transcription elongation with double-strand break repair at active promoters [ Mol Cell, 2021, 81(4):830-844.e13]	PubMed: 33453168
Ubiquitylation of MYC couples transcription elongation with double-strand break repair at active promoters [ Mol Cell, 2021, S1097-2765(20)30956-4]	PubMed: 33453168
MYC Recruits SPT5 to RNA Polymerase II to Promote Processive Transcription Elongation. [ Mol Cell, 2019, 74(4):674-687]	PubMed: 30928206

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。