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Chemical Structure| 1996629-79-8 Chemical Structure| 1996629-79-8

Structure of TBOPP
CAS No.: 1996629-79-8

Chemical Structure| 1996629-79-8

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TBOPP is a selective DOCK1 inhibitor with IC50 value of 8.4μM. It dampened DOCK1-mediated invasion, macropinocytosis, and survival under the condition of glutamine deprivation. TBOPP treatment suppressed cancer metastasis and growth in vivo in mice.

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Product Details of TBOPP

CAS No. :1996629-79-8
Formula : C24H21F3N2O4S
M.W : 490.49
SMILES Code : O=C1C=CC(S(=O)(N2CCCC2)=O)=CN1CC(C3=CC=C(C4=CC=CC(C(F)(F)F)=C4)C=C3)=O
MDL No. :MFCD32215320
InChI Key :ZMPDEBWNVHAKBB-UHFFFAOYSA-N
Pubchem ID :122508151

Safety of TBOPP

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
ACHN 0-40 µM 48 hours TBOPP decreased the viability and proliferation of ACHN cells Mol Med Rep. 2020 Aug;22(2):1187-1194
786-O 0-40 µM 48 hours TBOPP decreased the viability and proliferation of 786-O cells Mol Med Rep. 2020 Aug;22(2):1187-1194
JAR cells 10 µM 24 hours Inhibition of DOCK1 resulted in cell cycle arrest at G0/G1 phase and reduced S phase cell population Life Sci Alliance. 2023 Nov 15;7(2):e202302247
HTR-8/SVneo cells 10 µM 24 hours Inhibition of DOCK1 resulted in cell cycle arrest at G0/G1 phase and reduced S phase cell population Life Sci Alliance. 2023 Nov 15;7(2):e202302247
PLC cells 0.75 µM or 1 µM 48 hours TBOPP significantly inhibited RAC1 activation and showed strong synergistic anti-tumor effects when combined with metformin Protein Cell. 2022 Nov;13(11):825-841
Caki-1 0-40 µM 48 hours TBOPP decreased the viability and proliferation of Caki-1 cells Mol Med Rep. 2020 Aug;22(2):1187-1194
Patient-derived HCC organoids (1T and 2T) 1.5 µM and 7.5 µM 6 days Combined treatment of TBOPP and metformin significantly decreased cell viability in patient-derived HCC organoids Protein Cell. 2022 Nov;13(11):825-841

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice Pregnant mouse model Intraperitoneal injection 0.75 mg/mouse Administered on gestational days 6, 8, 10, and 12, continued until day 13.5 TBOPP treatment significantly increased the abortion rate in mice, elevated DUSP4 protein levels in placental tissues, and decreased phosphorylated ERK and HUWE1 levels Life Sci Alliance. 2023 Nov 15;7(2):e202302247
Mice PLC xenograft model Intravenous injection 8 mg/kg Twice a week, duration not specified 8 mg/kg TBOPP combined with 100 mg/kg metformin significantly suppressed PLC xenograft tumor growth Protein Cell. 2022 Nov;13(11):825-841

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.04mL

0.41mL

0.20mL

10.19mL

2.04mL

1.02mL

20.39mL

4.08mL

2.04mL

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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