TGX-221

Catalog No. A10923

TGX-221是PI3Kp110β的有效，选择性和细胞渗透性抑制剂。

Product Citations

Mostafa Khater, .et al. Gβγ translocation to the Golgi apparatus activates ARF1 to spatiotemporally regulate G protein-coupled receptor signaling to MAPK, J Biol Chem, 2021, Jan-Jun, 296:100805 PMID: 34022220
Mostafa Khater, .et al. G protein βγ translocation to the Golgi apparatus activates MAPK via p110γ-p101 heterodimers, J Biol Chem, 2021, Jan 22;296:100325 PMID: 33493514
Pridham KJ, .et al. PIK3CB/p110β is a selective survival factor for glioblastoma, Neuro Oncol, 2018, Mar 27;20(4):494-505 PMID: 29016844

Technical details

Catalog Num	A10923
M. Wt	364.4
Formula	C21H24N4O2
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	663619-89-4
Synonyms	TGX221
SMILES	CC1=CN2C(=O)C=C(N=C2C(=C1)C(C)NC3=CC=CC=C3)N4CCOCC4

Biological Activity

TGX-221是PI3Kp110β的有效，选择性和细胞渗透性抑制剂。

Targets

Target	Value
p110β	IC50: 5nM
p110δ	IC50: 0.1μM
p110α	IC50: 5μM
p110γ	IC50: >10μM
C2α	IC50: >10μM
PI4K	IC50: >10μM
Abl	IC50: >10μM
EGFR	IC50: >10μM
Fyn	IC50: >10μM
HER2	IC50: >10μM
Insulin Receptor	IC50: >10μM
CaseinKinase2	IC50: >10μM
CDK2/CyclinA	IC50: >10μM
ERK1	IC50: >10μM
p38α	IC50: >10μM
p70S6K	IC50: >10μM
PKA	IC50: >10μM
PKC	IC50: >10μM
CaMK	IC50: >10μM

Solubility *

In vitro (25°C)	DMSO	11 mg/mL (30.18 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	1% DMSO+30% polyethylene glycol+1% Tween 80	28 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq 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.

Preparing Stock Solutions

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	27.44 mL	137.21 mL	274.42 mL
0.5 mM	5.49 mL	27.44 mL	54.88 mL
1 mM	2.74 mL	13.72 mL	27.44 mL
5 mM	0.55 mL	2.74 mL	5.49 mL

*The above data is based on the productmolecular weight 364.4 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.