TGX-221

製品コードS1169 バッチS116901

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	C₂₁H₂₄N₄O₂
	分子量	364.44	CAS No.	663619-89-4
Solubility (25°C)*	体外	DMSO	12 mg/mL (32.92 mM)
		Water	Insoluble
		Ethanol	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	TGX-221 is a p110β-specific inhibitor with IC50 of 5 nM in a cell-free assay, 1000-fold more selective for p110β than p110α.
in vitro	The activity of TGX-221 against different isoforms is measured in an in vitro PI3K assay using multiple preparations of recombinant p85/p110. TGX-221 show slow potent to p110δ with IC50 of 211 nM. Furthermore, TGX-221 partially attenuates insulin-induced phosphorylation of Ser⁴⁷³ of PKB in J774.2 macrophage cells. ^[1] TGX-221 inhibits platelet-ECC interaction, platelet aggregation and platelet-granulocyte binding in an extracorporeal circulation (ECC) model. ^[2] A recent study shows that after treatment with TGX-221 (0.2, 2, and 20 μM), PC3 cells show inhibition of proliferation with a significant reduction of the activity of the p110β PI3K isoform. ^[3]
in vivo	As an anti-thrombotic agent, TGX-221 at doses 1 + 1 (49 %) and 3+3 (88 %) improves integrated blood flow over 30 minutes in a mouse model. In addition, Tail bleeding time (BT) (sec) increases with TGX-221 doses of 3 + 3 (median 1560) and 1 + 1 (1305) and mean renal BT (sec) also increases in all TGX-221 groups. ^[4]

プロトコル(参考用のみ)

キナーゼアッセイ	Lipid kinase activity
キナーゼアッセイ	IC50 values are measured using a standard lipid kinase activity with PI as a substrate. (i)100 μM cold ATP is used instead of 10 μM, (ii) the DMSO concentration is 1%, and (iii) [γ-³³P]ATP is used instead of [γ-³²P]ATP. The TLC plates are quantified using a phosphorimager screen. The reported IC50 values are determined by non-linear regression analysis on the basis of at least three independent experiments repeated across multiple preparations of recombinant protein.
細胞アッセイ	細胞株	PC3 cells
	濃度	~20 μM
	反応時間	24-72 hours
	実験の流れ	For measurement of proliferation, cells are seeded in triplicate in 96-well culture plates and incubated overnight to allow cell attachment. The cells are incubated with TGX-221 for 24, 48, and 72 hours. At designated time intervals, cells are quantified by a crystal violet staining-based colorimetric assay. Briefly, cells are fixed by addition of 100 μl of 2.5% glutaraldehyde solution and incubated at room temperature for 30 minutes. Plates are washed three times by submersion in PBS solution. Plates are air-dried and stained by addition of 100 μL of 0.1% solution of crystal violet dissolved in deionized water and incubated for 20 minutes at room temperature, excess dye is removed by extensive washing with deionized water, and plates are air-dried prior to bound dye solubilization in 100 μL of 10% acetic acid. The optical density of dye extracts is measured directly in plates using a microplate reader at 570 nm.
動物実験	動物モデル	FeCl3-induced arterial thrombosis in mice
	投薬量	0.3 + 0.3, 1 + 1, 3 + 3 mg/kg + mg/kg/hour
	投与方法	Administered via i.v.

参考

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カスタマーフィードバック

: Data from [Mol Med, 2012, 18, 336-45]

: Data from [Mol Med, 2012, 18, 336-45]

: Data from [Mol Med, 2012, 18, 336-45]

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：

Machine learning-based identification of lower grade glioma stemness subtypes discriminates patient prognosis and drug response [ Comput Struct Biotechnol J, 2023, 21:3827-3840]	PubMed: 37560125
Pan-PI3K inhibition with copanlisib overcomes Treg- and M2-TAM-mediated immune suppression and promotes anti-tumor immune responses [ Clin Exp Med, 2023, 10.1007/s10238-023-01227-6]	PubMed: 37935952
Overcoming resistance to immune checkpoint therapy in PTEN-null prostate cancer by intermittent anti-PI3Kα/β/δ treatment [ Nat Commun, 2022, 13(1):182]	PubMed: 35013322
Long noncoding RNA-mediated activation of PROTOR1/PRR5-AKT signaling shunt downstream of PI3K in triple-negative breast cancer [ Proc Natl Acad Sci U S A, 2022, 119(43):e2203180119]	PubMed: 36269860
Platelet p110β mediates platelet-leukocyte interaction and curtails bacterial dissemination in pneumococcal pneumonia [ Cell Rep, 2022, 41(6):111614]	PubMed: 36351402
The Lectin LecB Induces Patches with Basolateral Characteristics at the Apical Membrane to Promote Pseudomonas aeruginosa Host Cell Invasion [ mBio, 2022, 13(3):e0081922]	PubMed: 35491830
Upregulated Apelin Signaling in Pancreatic Cancer Activates Oncogenic Signaling Pathways to Promote Tumor Development [ Int J Mol Sci, 2022, 23-1810600]	PubMed: 36142542
The Pro-Fibrotic Response to Lens Injury Is Signaled in a PI3K Isoform-Specific Manner [ Biomolecules, 2022, 12-91181]	PubMed: 36139020
Whole-genome CRISPR screening identifies PI3K/AKT as a downstream component of the oncogenic GNAQ-Focal Adhesion Kinase signaling circuitry [ J Biol Chem, 2022, S0021-9258(22)01309-6]	PubMed: 36596361
Combined Treatment with PI3K Inhibitors BYL-719 and CAL-101 Is a Promising Antiproliferative Strategy in Human Rhabdomyosarcoma Cells [ Molecules, 2022, 27(9)2742]	PubMed: 35566091

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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