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Chemical Structure| 663619-89-4 Chemical Structure| 663619-89-4

Structure of TGX-221
CAS No.: 663619-89-4

Chemical Structure| 663619-89-4

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TGX-221 is a p110β-specific inhibitor with IC50 of 5 nM in a cell-free assay, and is 1000-fold selective for p110β than p110α.

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Product Details of TGX-221

CAS No. :663619-89-4
Formula : C21H24N4O2
M.W : 364.44
SMILES Code : O=C1C=C(N2CCOCC2)N=C3N1C=C(C)C=C3C(NC4=CC=CC=C4)C
MDL No. :MFCD11113209
InChI Key :CPRAGQJXBLMUEL-UHFFFAOYSA-N
Pubchem ID :9907093

Safety of TGX-221

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of TGX-221

PI3K-AKT

Isoform Comparison

Biological Activity

Target
  • p110β

    p110β, IC50:5 nM

  • p110δ

    p110δ, IC50:0.1 μM

In Vitro:

Cell Line
Concentration Treated Time Description References
Human NK cells 1 μM 2 hours To evaluate the effect of MLN1117 on human NK cell-mediated cytotoxicity. Results showed that selective inhibition of p110α had minimal impact on human NK cell-mediated cytotoxicity. PLoS One. 2014 Jun 10;9(6):e99486.
Natural Killer (NK) cells 0.5 μM 15 minutes To evaluate the effect of MLN1117 on NK cell-mediated cytotoxicity. Results showed that selective inhibition of p110α had minimal impact on NK cell-mediated cytotoxicity. PLoS One. 2014 Jun 10;9(6):e99486.
Primary microglia derived from wild-type mice 200 nM 6 days To investigate the effect of TGX-221 on LPS- or ATP-induced microglial proliferation, results showed that TGX-221 inhibited PI3Kβ activity but did not significantly affect microglial proliferation Cells. 2021 Sep 24;10(10):2534.
AR4-2J B13 cells 0.5 µM 5 days Treatment with TGX-221 prevented the DEX+EGF-induced F-actin relocalization and cell spreading, indicating the role of p110β in acinar cell transdifferentiation. Genes Dev. 2014 Dec 1;28(23):2621-35.
EFO21 cells 10 µM 72 h To evaluate the effect of TGX-221 on p85 β-overexpressing cells, results showed that TGX-221 significantly inhibited the p85 β-induced phenotypes Nat Commun. 2020 May 8;11(1):2291.
Mouse platelets 0.5 µM To investigate the effect of TGX-221 on the adhesion frequency of diabetic mouse platelets, results showed that TGX-221 suppressed the increment in the fibrinogen adhesion frequency observed in diabetic platelets after 50 s Nat Commun. 2018 Mar 14;9(1):1087.
Human platelets 0.5 µM To investigate the effect of TGX-221 on the adhesion frequency of diabetic human platelets, results showed that TGX-221 suppressed the increment in the fibrinogen adhesion frequency observed in diabetic platelets after 50 s Nat Commun. 2018 Mar 14;9(1):1087.
U-87 MG cells 20 μM 48 h TGX-221 did not significantly inhibit U-87 MG cell proliferation but reduced Akt phosphorylation levels. J Exp Clin Cancer Res. 2016 May 12;35:78.
U-373 MG cells 20 μM 48 h TGX-221 showed similar inhibitory effects in U-373 MG cells as in U-87 MG cells. J Exp Clin Cancer Res. 2016 May 12;35:78.
NIH3T3 cells 40 nM To investigate the effect of TGX-221 on MET-dependent cell migration, results showed that TGX-221 alone had no significant effect, but in combination with A66 significantly reduced the migration of METM1268T cells. Sci Signal. 2020 Jun 23;13(637):eaba8627.
U87MG cells 40 nM To investigate the effect of TGX-221 on U87MG cell migration, results showed that TGX-221 alone had no significant effect, but in combination with A66 significantly reduced the migration of U87MG cells. Sci Signal. 2020 Jun 23;13(637):eaba8627.
C2C12 cells 500 nM 1 h To investigate the inhibitory effect of TGX-221 on PI3K β, the results showed that TGX-221 did not affect the translocation of the Akt PH bioreporter induced by Vav2Onc. Nat Commun. 2020 Nov 16;11(1):5808.
DKO+p110β-wt MEFs 2 µM TGX-221 is a specific inhibitor of p110β, used to study the role of p110β in PI3K signaling. The results showed that TGX-221 inhibited Akt phosphorylation in p110β-wt MEFs. Elife. 2016 Oct 4;5:e17635.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mouse Diabetic mouse model Intravenous injection 2.5 mg/kg Single dose, lasting 10 minutes To investigate the effect of TGX-221 on thrombus formation in diabetic mice, results showed that TGX-221 significantly reduced the rate and stability of thrombus formation in diabetic mice Nat Commun. 2018 Mar 14;9(1):1087.
Balb/C nude mice U-87 MG glioblastoma xenograft model Intraperitoneal injection 40 mg/kg Once daily for 7 days Combination of TGX-221 with JNK inhibitor SP600125 significantly inhibited the growth of U-87 MG xenograft tumors. J Exp Clin Cancer Res. 2016 May 12;35:78.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.74mL

0.55mL

0.27mL

13.72mL

2.74mL

1.37mL

27.44mL

5.49mL

2.74mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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