umbralisib (TGR-1202)

製品コードS8194 バッチS819402

化学情報

	Synonyms	Rp-5264	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₃₁H₂₄F₃N₅O₃
	分子量	571.55	CAS No.	1532533-67-7
Solubility (25°C)*	体外	DMSO	100 mg/mL warmed with 50ºC water bath (174.96 mM)
		Ethanol	7 mg/mL warmed with 50ºC water bath (12.24 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	Umbralisib (TGR-1202, Rp-5264), a novel, next generation PI3Kδ inhibitor, inhibits PI3Kδ activity in enzyme and cell based assays with IC50 and EC50 values of 22.2 & 24.3 nM, respectively.
in vitro	The compound displays a high degree of selectivity over the alpha (>1000 fold), beta (>30-50 fold), and gamma (>15-50 fold) isoforms. Additionally, the compound causes a half-maximal inhibition of human whole blood CD19 cell proliferation between 100-300 nM. Treatment of PBMC with RP5264 results initially in a G2/M arrest followed by subsequent increase in the number of Sub G0 cells. Viability assays demonstrate that the compound causes a significant inhibition in growth as well as Akt phosphorylation of immortalized and primary leukemic cells^[1].
in vivo	The compound exhibits good oral absorption with favourable pharmacokinetic properties in rodents. It also has an excellent safety profile^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Multiple Myeloma resistant (MM-1R) or sensitive (MM-1S) cells
	濃度	--
	反応時間	96 h
	実験の流れ	Multiple Myeloma resistant (MM-1R) or sensitive (MM-1S) cells are incubated with desired concentrations of RP5264. Growth is assessed after 96 h by a MTT assay.
動物実験	動物モデル	Female Balb/c mice
	投薬量	12.5, 25, 50 mg/kg
	投与方法	oral administration

参考

[1] Swaroop Vakkalanka, et al. AACR Poster. 2012, Poster3741.

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：

Targeting IRAK4 with Emavusertib in Lymphoma Models with Secondary Resistance to PI3K and BTK Inhibitors [ J Clin Med, 2023, 12(2)399]	PubMed: 36675328
Functional Testing to Characterize and Stratify PI3K Inhibitor Responses in Chronic Lymphocytic Leukemia [ Clin Cancer Res, 2022, 28-20:4444-4455]	PubMed: 35998013
Resistance to PI3κδ inhibitors in marginal zone lymphoma can be reverted by targeting the IL-6/PDGFRA axis [ Haematologica, 2022, 10.3324/haematol.2021.279957]	PubMed: 35484662
The delta isoform of PI3K predominates in chronic myelomonocytic leukemia and can be targeted effectively with umbralisib and ruxolitinib [ Exp Hematol, 2021, S0301-472X(21)00089-8]	PubMed: 33617893
Ex vivo blockade of PI3K gamma or delta signaling enhances the antitumor potency of adoptively transferred CD8+ T cells. [ Eur J Immunol, 2020, 8]	PubMed: 32383488

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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