LDC4297

製品コードS7992 バッチS799201

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
* <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 LDC4297 for CDK7 proves to be extremely high. The replication of HCMV in cultured primary human fibroblasts (HFFs) is inhibited by LDC4297 in a concentration-dependent manner with a 50% effective concentration (EC50) value of 24.5 ± 1.3 nM. Notably, CDK7 inhibition by LDC4297 is not associated with general cytotoxicity at submicromolar concentrations. In contrast, LDC4297 induces cytotoxicity in a set of tumor cell lines, i.e., already at extremely low, nanomolar concentrations in specific cases. Anti-HCMV activity of LDC4297 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 LDC4297. 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 LDC4297 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

[1] Hutterer C, et al. Antimicrob Agents Chemother. 2015, 59(4):2062-71.

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：

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, 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。

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