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Chemical Structure| 1698055-85-4 Chemical Structure| 1698055-85-4

Structure of ARS-1620
CAS No.: 1698055-85-4

Chemical Structure| 1698055-85-4

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ARS-1620 is an atropisomeric selective KRASG12C inhibitor with desirable pharmacokinetics.

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Product Details of ARS-1620

CAS No. :1698055-85-4
Formula : C21H17ClF2N4O2
M.W : 430.84
SMILES Code : O=C(N1CCN(CC1)C2=C3C=C(Cl)C(C4=C(O)C=CC=C4F)=C(F)C3=NC=N2)C=C
MDL No. :MFCD31619312
InChI Key :ZRPZPNYZFSJUPA-UHFFFAOYSA-N
Pubchem ID :137003167

Safety of ARS-1620

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

Related Pathways of ARS-1620

GPCR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
H358 cells 0.05 μM, 0.1 μM, 0.3 μM 3 hours ARS-1620 disrupts the KRASG12C-AGO2 interaction PMC7272436
MIA PaCa-2 cells 2 μM, 4 μM, 8 μM 9 hours ARS-1620 disrupts the KRASG12C-AGO2 interaction PMC7272436
Panc 05.04 cells 2 μM, 4 μM, 8 μM 24 hours ARS-1620 had no effect on the KRASG12D-AGO2 interaction PMC7272436
Panc 10.05 cells 0.3 μM, 1.0 μM, 3 μM 24 hours ARS-1620 had no effect on the KRASG12D-AGO2 interaction PMC7272436
NCI-H358 cells 1 μM 6, 24, and 48 hours Analysis of signaling changes in KRASG12C cell lines after ARS-1620 treatment revealed that H358 cells were most sensitive to ARS-1620 with an IC50 of 0.4 μM. PMC9940280
Calu1 cells 1 μM 6, 24, and 48 hours Calu1 cells showed a moderate response to ARS-1620, with signaling analysis indicating rebound in pERK and pAkt suppression starting at 24 hours. PMC9940280
NCI-H1792 cells 1 μM 6, 24, and 48 hours H1792 cells exhibited strong resistance to ARS-1620, with signaling analysis showing rebound in pERK and pAkt suppression starting at 24 hours. PMC9940280
H23 cells 1 μM 24 hours Test the inhibitory effect of ARS-1620 alone or in combination with IGF1R and mTOR inhibitors on KRAS-G12C mutant cells, showing that the combination significantly enhanced the inhibition of cell proliferation. PMC6764843
H358 cells 1 μM 24 hours Test the inhibitory effect of ARS-1620 alone or in combination with IGF1R and mTOR inhibitors on KRAS-G12C mutant cells, showing that the combination significantly enhanced the inhibition of cell proliferation. PMC6764843
H1792 cells 1 μM 24 hours Test the inhibitory effect of ARS-1620 alone or in combination with IGF1R and mTOR inhibitors on KRAS-G12C mutant cells, showing that the combination significantly enhanced the inhibition of cell proliferation. PMC6764843

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice KRAS-G12C mutant lung cancer models Oral gavage or intraperitoneal administration 100 or 200 mg/kg 5 days per week for 3 weeks Test the inhibitory effect of ARS-1620 alone or in combination with IGF1R and mTOR inhibitors on KRAS-G12C mutant tumors, showing that the combination significantly enhanced the inhibition of tumor growth. PMC6764843

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.32mL

0.46mL

0.23mL

11.61mL

2.32mL

1.16mL

23.21mL

4.64mL

2.32mL

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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