TGX-221

Name: TGX-221
Brand: MedChemExpress
SKU: HY-10114
Rating: 5.0 (17 reviews)

Cat. No.: HY-10114 Purity: 99.45%: Data Sheet
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TGX-221 is a potent, selective, and cell membrane permeable inhibitor of the PI3K p110β catalytic subunit, used for cancer treatment.

For research use only. We do not sell to patients.

TGX-221 Chemical Structure

CAS No. : 663619-89-4

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10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 17 publication(s) in Google Scholar

Other Forms of TGX-221:

TGX-221 (Standard) Get quote

17 Publications Citing Use of MCE TGX-221

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All PI3K Isoform Specific Products:

View All Isoforms

PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

TGX-221 is a potent, selective, and cell membrane permeable inhibitor of the PI3K p110β catalytic subunit, used for cancer treatment.

IC₅₀ & Target^[5]

p110β

8.5 nM (IC₅₀)

p110δ

211 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
PC-3	IC₅₀	10 1 Compound: TGX-221	Inhibition of mTORC2-mediated Akt phosphorylation at Ser473 residue in PTEN-deficient human PC3 cells after 2 hrs by Western blot analysis Inhibition of mTORC2-mediated Akt phosphorylation at Ser473 residue in PTEN-deficient human PC3 cells after 2 hrs by Western blot analysis	[PMID: 22524426]
PC-3	IC₅₀	3 1 Compound: TGX-221	Inhibition of human PI3Kbeta-mediated Akt phosphorylation at T308 residue expressed in PTEN-deficient human PC3 cells after 2 hrs by Western blot analysis Inhibition of human PI3Kbeta-mediated Akt phosphorylation at T308 residue expressed in PTEN-deficient human PC3 cells after 2 hrs by Western blot analysis	[PMID: 22524426]
PC-3	IC₅₀	10 1 Compound: TGX-221	Inhibition of PI3Kbeta-mediated Akt phosphorylation at S473 in PTEN-deficient human PC3 cells after 0.5 to 2 hrs by Immunoblotting assay Inhibition of PI3Kbeta-mediated Akt phosphorylation at S473 in PTEN-deficient human PC3 cells after 0.5 to 2 hrs by Immunoblotting assay	[PMID: 24387221]
PC-3	IC₅₀	10 1 Compound: TGX-221	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]
PC-3	IC₅₀	10 1 Compound: TGX-221	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]
PC-3	IC₅₀	10 1 Compound: TGX-221	Inhibition of PI3Kbeta-mediated Akt phosphorylation at S473 in PTEN-deficient human PC3 cells after 0.5 to 2 hrs by Immunoblotting assay Inhibition of PI3Kbeta-mediated Akt phosphorylation at S473 in PTEN-deficient human PC3 cells after 0.5 to 2 hrs by Immunoblotting assay	[PMID: 24387221]
PC-3	IC₅₀	10 1 Compound: TGX-221	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]
PC-3	IC₅₀	10 1 Compound: TGX-221	Inhibition of mTORC2-mediated Akt phosphorylation at Ser473 residue in PTEN-deficient human PC3 cells after 2 hrs by Western blot analysis Inhibition of mTORC2-mediated Akt phosphorylation at Ser473 residue in PTEN-deficient human PC3 cells after 2 hrs by Western blot analysis	[PMID: 22524426]
PC-3	IC₅₀	3 1 Compound: TGX-221	Inhibition of human PI3Kbeta-mediated Akt phosphorylation at T308 residue expressed in PTEN-deficient human PC3 cells after 2 hrs by Western blot analysis Inhibition of human PI3Kbeta-mediated Akt phosphorylation at T308 residue expressed in PTEN-deficient human PC3 cells after 2 hrs by Western blot analysis	[PMID: 22524426]
Sf21	IC₅₀	30 1 Compound: TGX-221	Inhibition of N-terminal ploy-His-tagged human PI3Kbeta expressed in baculovirus-infected sf21 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay Inhibition of N-terminal ploy-His-tagged human PI3Kbeta expressed in baculovirus-infected sf21 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay	[PMID: 24387221]
Sf21	IC₅₀	52 1 Compound: TGX-221	Inhibition of PI3Kbeta (unknown origin) expressed in Escherichia coli-infected fall armyworm sf21 cells co-expressing p85 by kinase-glo luminescence assay Inhibition of PI3Kbeta (unknown origin) expressed in Escherichia coli-infected fall armyworm sf21 cells co-expressing p85 by kinase-glo luminescence assay	[PMID: 27387421]
RAW264.7	IC₅₀	> 1000 1 Compound: TGX-221	Inhibition of human PI3Kgamma-mediated Akt phosphorylation at Ser473 residue expressed in mouse RAW264.7 cells after 0.5 to 2 hrs by Western blot analysis Inhibition of human PI3Kgamma-mediated Akt phosphorylation at Ser473 residue expressed in mouse RAW264.7 cells after 0.5 to 2 hrs by Western blot analysis	[PMID: 22524426]
PC-3	IC₅₀	10 1 Compound: TGX-221	Inhibition of PI3Kbeta-mediated Akt phosphorylation at S473 in PTEN-deficient human PC3 cells after 0.5 to 2 hrs by Immunoblotting assay Inhibition of PI3Kbeta-mediated Akt phosphorylation at S473 in PTEN-deficient human PC3 cells after 0.5 to 2 hrs by Immunoblotting assay	[PMID: 24387221]
Sf21	IC₅₀	63 1 Compound: TGX-221	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	30 1 Compound: TGX-221	Inhibition of N-terminal ploy-His-tagged human PI3Kbeta expressed in baculovirus-infected sf21 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay Inhibition of N-terminal ploy-His-tagged human PI3Kbeta expressed in baculovirus-infected sf21 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay	[PMID: 24387221]
PC-3	IC₅₀	3 1 Compound: TGX-221	Inhibition of human PI3Kbeta-mediated Akt phosphorylation at T308 residue expressed in PTEN-deficient human PC3 cells after 2 hrs by Western blot analysis Inhibition of human PI3Kbeta-mediated Akt phosphorylation at T308 residue expressed in PTEN-deficient human PC3 cells after 2 hrs by Western blot analysis	[PMID: 22524426]
RAW264.7	IC₅₀	>1 3 Compound: TGX-221	Inhibition of human PI3Kgamma-mediated Akt phosphorylation at Ser473 residue expressed in mouse RAW264.7 cells after 0.5 to 2 hrs by Western blot analysis Inhibition of human PI3Kgamma-mediated Akt phosphorylation at Ser473 residue expressed in mouse RAW264.7 cells after 0.5 to 2 hrs by Western blot analysis	[PMID: 22524426]
Sf21	IC₅₀	52 1 Compound: TGX-221	Inhibition of PI3Kbeta (unknown origin) expressed in Escherichia coli-infected fall armyworm sf21 cells co-expressing p85 by kinase-glo luminescence assay Inhibition of PI3Kbeta (unknown origin) expressed in Escherichia coli-infected fall armyworm sf21 cells co-expressing p85 by kinase-glo luminescence assay	[PMID: 27387421]
RAW264.7	IC₅₀	> 1000 1 Compound: TGX-221	Inhibition of human PI3Kgamma-mediated Akt phosphorylation at Ser473 residue expressed in mouse RAW264.7 cells after 0.5 to 2 hrs by Western blot analysis Inhibition of human PI3Kgamma-mediated Akt phosphorylation at Ser473 residue expressed in mouse RAW264.7 cells after 0.5 to 2 hrs by Western blot analysis	[PMID: 22524426]
Sf21	IC₅₀	30 1 Compound: TGX-221	Inhibition of N-terminal ploy-His-tagged human PI3Kbeta expressed in baculovirus-infected sf21 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay Inhibition of N-terminal ploy-His-tagged human PI3Kbeta expressed in baculovirus-infected sf21 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay	[PMID: 24387221]
Sf9	IC₅₀	851 1 Compound: TGX-221	Inhibition of N-terminal ploy-His-tagged human PI3Kdelta expressed in baculovirus-infected sf9 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay Inhibition of N-terminal ploy-His-tagged human PI3Kdelta expressed in baculovirus-infected sf9 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay	[PMID: 24387221]
Sf21	IC₅₀	63 1 Compound: TGX-221	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]
Sf9	IC₅₀	> 10000 1 Compound: TGX-221	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	851 1 Compound: TGX-221	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]
Sf21	IC₅₀	52 1 Compound: TGX-221	Inhibition of PI3Kbeta (unknown origin) expressed in Escherichia coli-infected fall armyworm sf21 cells co-expressing p85 by kinase-glo luminescence assay Inhibition of PI3Kbeta (unknown origin) expressed in Escherichia coli-infected fall armyworm sf21 cells co-expressing p85 by kinase-glo luminescence assay	[PMID: 27387421]
Sf21	IC₅₀	63 1 Compound: TGX-221	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]
Sf9	IC₅₀	10 3 Compound: TGX-221	Inhibition of C-terminal ploy-His-tagged human PI3Kgamma expressed in baculovirus-infected sf9 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay Inhibition of C-terminal ploy-His-tagged human PI3Kgamma expressed in baculovirus-infected sf9 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay	[PMID: 24387221]
Sf9	IC₅₀	> 10000 1 Compound: TGX-221	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	1 3 Compound: 1a, TGX-221	Inhibition of N-terminal His-tagged human p110alpha expressed in Sf9 cells co-expressing p85alpha regulatory subunit using phosphatidylinositol substrate and [gamma-33P]-ATP by basic thin layer chromatography technique based lipid kinase assay Inhibition of N-terminal His-tagged human p110alpha expressed in Sf9 cells co-expressing p85alpha regulatory subunit using phosphatidylinositol substrate and [gamma-33P]-ATP by basic thin layer chromatography technique based lipid kinase assay	[PMID: 25890698]
Sf9	IC₅₀	0.004 3 Compound: 1a, TGX-221	Inhibition of N-terminal His-tagged human p110beta expressed in Sf9 cells co-expressing p85alpha regulatory subunit using phosphatidylinositol substrate and [gamma-33P]-ATP by basic thin layer chromatography technique based lipid kinase assay Inhibition of N-terminal His-tagged human p110beta expressed in Sf9 cells co-expressing p85alpha regulatory subunit using phosphatidylinositol substrate and [gamma-33P]-ATP by basic thin layer chromatography technique based lipid kinase assay	[PMID: 25890698]
Sf9	IC₅₀	0.004 3 Compound: 1a, TGX-221	Inhibition of N-terminal His-tagged human p110beta expressed in Sf9 cells co-expressing p85alpha regulatory subunit using phosphatidylinositol substrate and [gamma-33P]-ATP by basic thin layer chromatography technique based lipid kinase assay Inhibition of N-terminal His-tagged human p110beta expressed in Sf9 cells co-expressing p85alpha regulatory subunit using phosphatidylinositol substrate and [gamma-33P]-ATP by basic thin layer chromatography technique based lipid kinase assay	[PMID: 25890698]
Sf9	IC₅₀	0.14 3 Compound: 1a, TGX-221	Inhibition of N-terminal His-tagged human p110delta expressed in Sf9 cells co-expressing p85alpha regulatory subunit using phosphatidylinositol substrate and [gamma-33P]-ATP by basic thin layer chromatography technique based lipid kinase assay Inhibition of N-terminal His-tagged human p110delta expressed in Sf9 cells co-expressing p85alpha regulatory subunit using phosphatidylinositol substrate and [gamma-33P]-ATP by basic thin layer chromatography technique based lipid kinase assay	[PMID: 25890698]
Sf9	IC₅₀	0.004 3 Compound: 1a, TGX-221	Inhibition of N-terminal His-tagged human p110beta expressed in Sf9 cells co-expressing p85alpha regulatory subunit using phosphatidylinositol substrate and [gamma-33P]-ATP by basic thin layer chromatography technique based lipid kinase assay Inhibition of N-terminal His-tagged human p110beta expressed in Sf9 cells co-expressing p85alpha regulatory subunit using phosphatidylinositol substrate and [gamma-33P]-ATP by basic thin layer chromatography technique based lipid kinase assay	[PMID: 25890698]
Sf9	IC₅₀	0.14 3 Compound: 1a, TGX-221	Inhibition of N-terminal His-tagged human p110delta expressed in Sf9 cells co-expressing p85alpha regulatory subunit using phosphatidylinositol substrate and [gamma-33P]-ATP by basic thin layer chromatography technique based lipid kinase assay Inhibition of N-terminal His-tagged human p110delta expressed in Sf9 cells co-expressing p85alpha regulatory subunit using phosphatidylinositol substrate and [gamma-33P]-ATP by basic thin layer chromatography technique based lipid kinase assay	[PMID: 25890698]
Sf9	IC₅₀	0.14 3 Compound: 1a, TGX-221	Inhibition of N-terminal His-tagged human p110delta expressed in Sf9 cells co-expressing p85alpha regulatory subunit using phosphatidylinositol substrate and [gamma-33P]-ATP by basic thin layer chromatography technique based lipid kinase assay Inhibition of N-terminal His-tagged human p110delta expressed in Sf9 cells co-expressing p85alpha regulatory subunit using phosphatidylinositol substrate and [gamma-33P]-ATP by basic thin layer chromatography technique based lipid kinase assay	[PMID: 25890698]
Sf9	IC₅₀	1 3 Compound: 1a, TGX-221	Inhibition of N-terminal His-tagged human p110alpha expressed in Sf9 cells co-expressing p85alpha regulatory subunit using phosphatidylinositol substrate and [gamma-33P]-ATP by basic thin layer chromatography technique based lipid kinase assay Inhibition of N-terminal His-tagged human p110alpha expressed in Sf9 cells co-expressing p85alpha regulatory subunit using phosphatidylinositol substrate and [gamma-33P]-ATP by basic thin layer chromatography technique based lipid kinase assay	[PMID: 25890698]
Sf9	IC₅₀	1 3 Compound: 1a, TGX-221	Inhibition of N-terminal His-tagged human p110alpha expressed in Sf9 cells co-expressing p85alpha regulatory subunit using phosphatidylinositol substrate and [gamma-33P]-ATP by basic thin layer chromatography technique based lipid kinase assay Inhibition of N-terminal His-tagged human p110alpha expressed in Sf9 cells co-expressing p85alpha regulatory subunit using phosphatidylinositol substrate and [gamma-33P]-ATP by basic thin layer chromatography technique based lipid kinase assay	[PMID: 25890698]
Sf9	IC₅₀	10000 1 Compound: TGX-221	Inhibition of C-terminal ploy-His-tagged human PI3Kgamma expressed in baculovirus-infected sf9 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay Inhibition of C-terminal ploy-His-tagged human PI3Kgamma expressed in baculovirus-infected sf9 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay	[PMID: 24387221]
Sf9	IC₅₀	>10 3 Compound: TGX-221	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 1 Compound: TGX-221	Inhibition of C-terminal ploy-His-tagged human PI3Kgamma expressed in baculovirus-infected sf9 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay Inhibition of C-terminal ploy-His-tagged human PI3Kgamma expressed in baculovirus-infected sf9 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay	[PMID: 24387221]
Sf9	IC₅₀	10000 1 Compound: TGX-221	Inhibition of N-terminal ploy-His-tagged human PI3Kalpha expressed in baculovirus-infected sf9 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay Inhibition of N-terminal ploy-His-tagged human PI3Kalpha expressed in baculovirus-infected sf9 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay	[PMID: 24387221]
Sf9	IC₅₀	10000 1 Compound: TGX-221	Inhibition of N-terminal ploy-His-tagged human PI3Kalpha expressed in baculovirus-infected sf9 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay Inhibition of N-terminal ploy-His-tagged human PI3Kalpha expressed in baculovirus-infected sf9 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay	[PMID: 24387221]
Sf9	IC₅₀	851 1 Compound: TGX-221	Inhibition of N-terminal ploy-His-tagged human PI3Kdelta expressed in baculovirus-infected sf9 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay Inhibition of N-terminal ploy-His-tagged human PI3Kdelta expressed in baculovirus-infected sf9 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay	[PMID: 24387221]
Sf9	IC₅₀	851 1 Compound: TGX-221	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]
Sf9	IC₅₀	851 1 Compound: TGX-221	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]
Sf9	IC₅₀	851 1 Compound: TGX-221	Inhibition of N-terminal ploy-His-tagged human PI3Kdelta expressed in baculovirus-infected sf9 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay Inhibition of N-terminal ploy-His-tagged human PI3Kdelta expressed in baculovirus-infected sf9 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay	[PMID: 24387221]
Sf9	IC₅₀	> 10000 1 Compound: TGX-221	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 1 Compound: TGX-221	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]

In Vitro

TGX-221, BL05 and BL05-HA show selective cytotoxicity to LNCaP cells, which may be due to the deficiency of PTEN in this cell line and the accumulation of PIP3 in the cells^[1].
TGX-221 (1 μM) does not affect the expression and phosphorylation of AMPK in C2C12 myoblasts^[2].
TGX221 (0.1, 1, 10 μM) induces IL-6 release from ASM cells^[2].
TGX-221 does not affect neurotensin-stimulated Akt phosphorylation when used alone, but it further suppresses neurotensin-stimulated phosphorylation of Akt when combined with gefitinib. TGX-221 abolishes the neurotensin-stimulated phosphorylation of Akt in Panc-1 cells^[3].

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

In Vivo

TGX-221 (TGX221, 2.5 mg/kg i.v.) abolishes cyclic flow reductions in a Folts-like carotid artery stenosis preparation of thrombosis, without changing bleeding time, heart rate, blood pressure or carotid vascular conductance^[4].

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

Molecular Weight

364.44

Formula

C₂₁H₂₄N₄O₂

CAS No.

663619-89-4

Appearance

Solid

Color

White to yellow

SMILES

O=C1N2C(C(C(NC3=CC=CC=C3)C)=CC(C)=C2)=NC(N4CCOCC4)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Solvent & Solubility

In Vitro:

DMSO : 12.5 mg/mL (34.30 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.7439 mL	13.7197 mL	27.4394 mL
5 mM	0.5488 mL	2.7439 mL	5.4879 mL
10 mM	0.2744 mL	1.3720 mL	2.7439 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (3.43 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.25 mg/mL (3.43 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1.25 mg/mL (3.43 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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mg/kg

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(per animal)

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(per animal)

μL

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.59%

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Data Sheet (284 KB) SDS (393 KB)

COA (252 KB) LCMS (336 KB)

Handling Instructions (2659 KB)

References

[1]. Zhao Y, et al. Prodrug strategy for PSMA-targeted delivery of TGX-221 to prostate cancer cells. Mol Pharm. 2012 Jun 4;9(6):1705-16. [Content Brief]

[2]. Sturgeon SA, et al. Advantages of a selective beta-isoform phosphoinositide 3-kinase antagonist, an anti-thrombotic agent devoid of other cardiovascular actions in the rat. Eur J Pharmacol. 2008 Jun 10;587(1-3):209-15. [Content Brief]

[3]. Ge Q, et al. The phosphoinositide 3'-kinase p110δ modulates contractile protein production and IL-6 release in human airway smooth muscle. J Cell Physiol. 2012 Aug;227(8):3044-52. [Content Brief]

[4]. Chaussade C, et al. Evidence for functional redundancy of class IA PI3K isoforms in insulin signalling. Biochem J. 2007 Jun 15;404(3):449-58. [Content Brief]

[5]. Müller KM, et al. Role of protein kinase C and epidermal growth factor receptor signalling in growth stimulation by neurotensin in colon carcinoma cells. BMC Cancer. 2011 Oct 2;11:421. [Content Brief]

Cell Assay ^[1]	The prostate cancer cell lines DU145 and LNCaP are maintained in RPMI-1640 medium, and PC3 cells are maintained in F-12K medium. LNCaP is a PSMA positive cell line, whereas DU145 and PC3 are PSMA negative. Both are supplemented with 10 % fetal bovine serum. Cells are plated in 96-well flat-bottomed plates at a concentration of 5,000 cells per well in 90 μL of growth medium. After 12 h, TGX-221, BL05, or BL05-HA loaded micelles in PBS are added at concentrations of 0, 0.1, 1, 5, 10, 50 or 100 μM. PBS and 10 μL of trichloroacetic acid (TCA) are added to negative and positive control wells, respectively. After 72 h, 10 μL of 55-μM resazurin blue is added to each well and incubated at 37°C for 4 h. After incubation, the resorufin product is measured with a fluorophotometer using an excitation wavelength of 560 nm and an emission wavelength of 590 nm. The IC₅₀ is determined as the midpoint between positive and negative control groups for each plate using GraphPad Prism 5 software. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[4]	Rats are randomLy assigned to drug treatment groups consisting of the vehicle propylene glycol (0.25 mL/kg), LY294002 (2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one; a reversible non-specific PI3K inhibitor; 10 mg/kg), wortmannin (an irreversible non-specific PI3K inhibitor; 5 mg/kg), IC87114 (2-[(6-aminopurin- 9-yl)methyl]-5-methyl-3-(2-methylphenyl)quinazolin-4-one; a PI3K p110δ antagonist; 2.5 mg/kg) and the selective PI3K p110β antagonist TGX221 (2.5 mg/kg). In the tail bleeding experiments, rats are randomLy assigned to drug treatment groups consisting of LY294002 (10 mg/kg), IC87114 (2.5 mg/kg), wortmannin (5 mg/kg), TGX221 (2.5 or 25 mg/kg), heparin (100 U/kg), aspirin (2× 200 mg/kg p.o.)± heparin (100 U/kg), and aspirin (2× 200 mg/kg p.o.) combined with heparin (100 U/kg) and TGX221 (2.5 mg/kg). All drugs, with the exception of aspirin, are administered as a slow (over ≈45-60 s) i.v. bolus of 0.25 mL/kg into the jugular vein. Aspirin (200 mg/kg suspended in 15% gum arabic in water) is administered twice orally (p.o.)-the first dose is given 24 h before the experiment and the second dose 1 h before the start of the experiment. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Zhao Y, et al. Prodrug strategy for PSMA-targeted delivery of TGX-221 to prostate cancer cells. Mol Pharm. 2012 Jun 4;9(6):1705-16. [Content Brief] [2]. Sturgeon SA, et al. Advantages of a selective beta-isoform phosphoinositide 3-kinase antagonist, an anti-thrombotic agent devoid of other cardiovascular actions in the rat. Eur J Pharmacol. 2008 Jun 10;587(1-3):209-15. [Content Brief] [3]. Ge Q, et al. The phosphoinositide 3'-kinase p110δ modulates contractile protein production and IL-6 release in human airway smooth muscle. J Cell Physiol. 2012 Aug;227(8):3044-52. [Content Brief] [4]. Chaussade C, et al. Evidence for functional redundancy of class IA PI3K isoforms in insulin signalling. Biochem J. 2007 Jun 15;404(3):449-58. [Content Brief] [5]. Müller KM, et al. Role of protein kinase C and epidermal growth factor receptor signalling in growth stimulation by neurotensin in colon carcinoma cells. BMC Cancer. 2011 Oct 2;11:421. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.7439 mL	13.7197 mL	27.4394 mL	68.5984 mL
	5 mM	0.5488 mL	2.7439 mL	5.4879 mL	13.7197 mL
	10 mM	0.2744 mL	1.3720 mL	2.7439 mL	6.8598 mL
	15 mM	0.1829 mL	0.9146 mL	1.8293 mL	4.5732 mL
	20 mM	0.1372 mL	0.6860 mL	1.3720 mL	3.4299 mL
	25 mM	0.1098 mL	0.5488 mL	1.0976 mL	2.7439 mL
	30 mM	0.0915 mL	0.4573 mL	0.9146 mL	2.2866 mL

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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-221663619-89-4TGX221TGX 221PI3KPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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TGX-221

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