TGX-155 (Synonyms: AZ12649385)

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TGX-155 (AZ12649385) is a selective inhibitor of PI3Kβ. TGX-155 has potential applications in antithrombotic therapy.

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TGX-155 Chemical Structure

CAS No. : 351071-90-4

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

Biological Activity
Purity & Documentation
References
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Description

TGX-155 (AZ12649385) is a selective inhibitor of PI3Kβ. TGX-155 has potential applications in antithrombotic therapy^[1]^[2]^[3].

IC₅₀ & Target^[1]

PI3Kβ

Cellular Effect

Cell Line	Type	Value	Description	References
PC-3	IC₅₀	72 nM Compound: TGX-155	Inhibition of human PI3Kbeta-mediated Akt phosphorylation at Ser473 residue expressed in PTEN-deficient human PC3 cells by chemiluminescence assay Inhibition of human PI3Kbeta-mediated Akt phosphorylation at Ser473 residue expressed in PTEN-deficient human PC3 cells by chemiluminescence assay	[PMID: 22524426]
Sf9	IC₅₀	> 10000 nM Compound: TGX-155	Inhibition of N-terminus poly-His tagged human PI3Kalpha expressed in baculovirus infected insect sf9 cells coexpressing p85alpha using PI(4,5)P2 as substrate preincubated with compound for 15 mins measured after 10 mins by HTRF assay Inhibition of N-terminus poly-His tagged human PI3Kalpha expressed in baculovirus infected insect sf9 cells coexpressing p85alpha using PI(4,5)P2 as substrate preincubated with compound for 15 mins measured after 10 mins by HTRF assay	[PMID: 22524426]
Sf9	IC₅₀	> 10000 nM Compound: TGX-155	Inhibition of N-terminus poly-His tagged human PI3Kgamma expressed in baculovirus infected insect sf9 cells using PI(4,5)P2 as substrate preincubated with compound for 15 mins measured after 10 mins by HTRF assay Inhibition of N-terminus poly-His tagged human PI3Kgamma expressed in baculovirus infected insect sf9 cells using PI(4,5)P2 as substrate preincubated with compound for 15 mins measured after 10 mins by HTRF assay	[PMID: 22524426]
Sf9	IC₅₀	166 nM Compound: TGX-155	Inhibition of poly-His tagged human PI3Kdelta expressed in baculovirus infected insect sf9 cells coexpressing p85alpha using PI(4,5)P2 as substrate preincubated with compound for 15 mins measured after 10 mins by HTRF assay Inhibition of poly-His tagged human PI3Kdelta expressed in baculovirus infected insect sf9 cells coexpressing p85alpha using PI(4,5)P2 as substrate preincubated with compound for 15 mins measured after 10 mins by HTRF assay	[PMID: 22524426]

In Vivo

TGX-155 (1.5 mg/kg and 2.5 mg/kg; i.v.; single dose) significantly improves the cyclic flow reductions (CFRs) in rabbit carotid artery injury in a time-dependent and dose-dependent manner^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

354.37

Formula

C₂₀H₁₉FN₂O₃

CAS No.

351071-90-4

SMILES

O=C1C2=CC=CC(OC3=C(C=C(F)C=C3)C)=C2NC(N4CCOCC4)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Verheijen J C, et al. Phosphatidylinositol 3-kinase (PI3K) inhibitors as anticancer drugs[J]. Drugs Future, 2007, 32(6): 537-547.

[2]. Nylander S, et al. Human target validation of phosphoinositide 3-kinase (PI3K)β: effects on platelets and insulin sensitivity, using AZD6482 a novel PI3Kβ inhibitor. J Thromb Haemost. 2012 Oct;10(10):2127-36. [Content Brief]

[3]. Sturgeon SA, et al. Adaptation of the Folts and electrolytic methods of arterial thrombosis for the study of anti-thrombotic molecules in small animals. J Pharmacol Toxicol Methods. 2006 Jan-Feb;53(1):20-9. [Content Brief]

TGX-155 Related Classifications

Cardiovascular Disease

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TGX-155351071-90-4AZ12649385TGX155TGX 155AZ 12649385AZ-12649385PI3KPhosphoinositide 3-kinaseRabbitCyclic flow reductionsCFRsInhibitorinhibitorinhibit

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