PI3Kβ-IN-1

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PI3Kβ-IN-1 (compound (P)-14) is a selective and orally active PI3Kβ inhibitor, with an IC₅₀ of 2 nM.

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PI3Kβ-IN-1 Chemical Structure

CAS No. : 2215098-77-2

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•Related Small Molecules:

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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

PI3Kβ-IN-1 (compound (P)-14) is a selective and orally active PI3Kβ inhibitor, with an IC₅₀ of 2 nM^[1].

IC₅₀ & Target

IC50: 2 nM (PI3Kβ)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
LNCaP	EC₅₀	24 nM Compound: (P)-14	Inhibition of PI3Kbeta in PTEN-deficient human LNCaP C4-2 cells assessed as reduction in AKT phosphorylation at Ser473 residue after 2 hrs by mesoscale assay Inhibition of PI3Kbeta in PTEN-deficient human LNCaP C4-2 cells assessed as reduction in AKT phosphorylation at Ser473 residue after 2 hrs by mesoscale assay	[PMID: 32551006]
LNCaP	EC₅₀	31 nM Compound: (P)-14	Inhibition of PI3Kbeta in PTEN-deficient human LNCAP cells assessed as reduction in AKT phosphorylation at Ser473 residue after 2 hrs by mesoscale assay Inhibition of PI3Kbeta in PTEN-deficient human LNCAP cells assessed as reduction in AKT phosphorylation at Ser473 residue after 2 hrs by mesoscale assay	[PMID: 32551006]
MDA-MB-415	EC₅₀	15 nM Compound: (P)-14	Inhibition of PI3Kbeta in PTEN-deficient human MDA-MB-415 cells assessed as reduction in AKT phosphorylation at Ser473 residue after 2 hrs by mesoscale assay Inhibition of PI3Kbeta in PTEN-deficient human MDA-MB-415 cells assessed as reduction in AKT phosphorylation at Ser473 residue after 2 hrs by mesoscale assay	[PMID: 32551006]
PC-3	EC₅₀	12 nM Compound: (P)-14	Inhibition of PI3Kbeta in PTEN-deficient human PC3 cells assessed as reduction in AKT phosphorylation at Ser473 residue after 2 hrs by mesoscale assay Inhibition of PI3Kbeta in PTEN-deficient human PC3 cells assessed as reduction in AKT phosphorylation at Ser473 residue after 2 hrs by mesoscale assay	[PMID: 32551006]
Sf21	IC₅₀	2 nM Compound: (P)-14	Inhibition of recombinant human full-length N-terminal His6-tagged p110beta/human recombinant full-length untagged p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate after 30 mins in presence of ATP at 2xKm concentration Inhibition of recombinant human full-length N-terminal His6-tagged p110beta/human recombinant full-length untagged p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate after 30 mins in presence of ATP at 2xKm concentration	[PMID: 32551006]
Sf21	IC₅₀	4 nM Compound: Rac-14	Inhibition of recombinant human full-length N-terminal His6-tagged p110beta/human recombinant full-length untagged p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate after 30 mins in presence of ATP at 2xKm concentration Inhibition of recombinant human full-length N-terminal His6-tagged p110beta/human recombinant full-length untagged p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate after 30 mins in presence of ATP at 2xKm concentration	[PMID: 32551006]
Sf21	IC₅₀	562 nM Compound: (M)-14	Inhibition of recombinant human full-length N-terminal His6-tagged p110beta/human recombinant full-length untagged p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate after 30 mins in presence of ATP at 2xKm concentration Inhibition of recombinant human full-length N-terminal His6-tagged p110beta/human recombinant full-length untagged p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate after 30 mins in presence of ATP at 2xKm concentration	[PMID: 32551006]
ZR-75-1	EC₅₀	5 nM Compound: (P)-14	Inhibition of PI3Kbeta in PTEN-deficient human ZR-75-1 cells assessed as reduction in AKT phosphorylation at Ser473 residue after 2 hrs by mesoscale assay Inhibition of PI3Kbeta in PTEN-deficient human ZR-75-1 cells assessed as reduction in AKT phosphorylation at Ser473 residue after 2 hrs by mesoscale assay	[PMID: 32551006]

Molecular Weight

464.43

Formula

C₂₅H₁₄F₂N₈

CAS No.

2215098-77-2

SMILES

CC([N@](C1=C2)[C@]3=CC=NC4=C(F)C=CC(F)=C34)=NC1=C(C5=NN=CN5)C=C2C6=CC=NC(C#N)=C6

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]. Perreault S, et al. Discovery of an Atropisomeric PI3Kβ Selective Inhibitor through Optimization of the Hinge Binding Motif. ACS Med Chem Lett. 2020 Apr 13;11(6):1236-1243. [Content Brief]

PI3Kβ-IN-1 Related Classifications

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

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The dilution calculator equation

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:

PI3Kβ-IN-12215098-77-2PI3KPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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