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Chemical Structure| 1648863-90-4 Chemical Structure| 1648863-90-4

Structure of G-5555
CAS No.: 1648863-90-4

Chemical Structure| 1648863-90-4

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G-5555 is a selective PAK1 inhibitor (Ki=3.7 nM).

4.5 *For Research Use Only !

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Product Details of G-5555

CAS No. :1648863-90-4
Formula : C25H25ClN6O3
M.W : 492.96
SMILES Code : ClC(C=C(C1=NC(C)=CC=C1)C=C2)=C2C3=CC4=CN=C(NC)N=C4N(C[C@@H]5OC[C@@H](N)CO5)C3=O
MDL No. :MFCD28506227

Safety of G-5555

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

Related Pathways of G-5555

cytoskeleton

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
THJ-16T 2.60 μM 72 hours To evaluate the effect of G-5555 on thyroid cancer cell viability, results showed that G-5555 significantly reduced cell viability Endocr Relat Cancer. 2019 Aug;26(8):699-712
FTC133 >10 μM 72 hours To evaluate the effect of G-5555 on thyroid cancer cell viability, results showed that G-5555 had minimal effect on FTC133 cell viability Endocr Relat Cancer. 2019 Aug;26(8):699-712
K1 6.98 μM 72 hours To evaluate the effect of G-5555 on thyroid cancer cell viability, results showed that G-5555 significantly reduced cell viability Endocr Relat Cancer. 2019 Aug;26(8):699-712
8505C 6.64 μM 72 hours To evaluate the effect of G-5555 on thyroid cancer cell viability, results showed that G-5555 significantly reduced cell viability Endocr Relat Cancer. 2019 Aug;26(8):699-712
SW1736 1.37 μM 72 hours To evaluate the effect of G-5555 on thyroid cancer cell viability, results showed that G-5555 significantly reduced cell viability Endocr Relat Cancer. 2019 Aug;26(8):699-712
HTh74 3.36 μM 72 hours To evaluate the effect of G-5555 on thyroid cancer cell viability, results showed that G-5555 significantly reduced cell viability Endocr Relat Cancer. 2019 Aug;26(8):699-712
BCPAP 2.46 μM 72 hours To evaluate the effect of G-5555 on thyroid cancer cell viability, results showed that G-5555 significantly reduced cell viability Endocr Relat Cancer. 2019 Aug;26(8):699-712
TPC1 0.50 μM 72 hours To evaluate the effect of G-5555 on thyroid cancer cell viability, results showed that G-5555 significantly reduced cell viability Endocr Relat Cancer. 2019 Aug;26(8):699-712
CMK cells 0.03, 0.1, 1, 3, 9, 20μmol/L 48 hours Inhibited CMK cell proliferation, 0.03 and 1μmol/L G5555 significantly inhibited CMK cell proliferation; 3μmol/L G5555 had a weaker inhibitory effect on CMK cell cycle; induced apoptosis, 3μmol/L G5555 increased the apoptosis rate of CMK cells by 2%. Zhonghua Xue Ye Xue Za Zhi. 2022 Jun 14;43(6):499-505
CHRF cells 0.03, 0.1, 1, 3, 9, 20μmol/L 48 hours Inhibited CHRF cell proliferation, 0.03 and 1μmol/L G5555 significantly inhibited CHRF cell proliferation; 3μmol/L G5555 reduced the percentage of CHRF cells in S phase from 37% to 15%; induced apoptosis, 3μmol/L G5555 increased the apoptosis rate of CHRF cells by 6.5%. Zhonghua Xue Ye Xue Za Zhi. 2022 Jun 14;43(6):499-505
Madin-Darby canine kidney epithelial cells 10 μM 60 minutes Measure compound permeability ACS Med Chem Lett. 2015 Oct 31;6(12):1241-6

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Thyroid-specific inducible BRAFV600E overexpression mouse model Oral gavage 25 mg/kg Twice daily for a week To evaluate the effect of G-5555 on BRAFV600E-induced thyroid cancer, results showed that G-5555 significantly restrained thyroid size and reduced carcinoma formation Endocr Relat Cancer. 2019 Aug;26(8):699-712
Nude mice H292 NSCLC xenograft model Oral 10, 20, 30 mg/kg Single dose, tumors and blood collected 6 hours postdose Study the effect of drug dose and exposure on pharmacodynamic biomarker pMEK S298 ACS Med Chem Lett. 2015 Oct 31;6(12):1241-6

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.03mL

0.41mL

0.20mL

10.14mL

2.03mL

1.01mL

20.29mL

4.06mL

2.03mL

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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