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Chemical Structure| 2446480-97-1 Chemical Structure| 2446480-97-1

Structure of KSQ-4279
CAS No.: 2446480-97-1

Chemical Structure| 2446480-97-1

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KSQ-4279 is a USP1 inhibitor that selectively inhibits USP1 activity, interfering with DNA repair processes. It shows potential therapeutic effects in cancer research, especially against tumor drug resistance.

Synonyms: USP1-IN-1

4.5 *For Research Use Only !

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Product Details of KSQ-4279

CAS No. :2446480-97-1
Formula : C27H25F3N8O
M.W : 534.54
SMILES Code : FC(C1=CN(C(C)C)C(C2=CC=C(CN3N=CC4=CN=C(C5=C(OC)N=CN=C5C6CC6)N=C43)C=C2)=N1)(F)F
Synonyms :
USP1-IN-1
MDL No. :N/A

Safety of KSQ-4279

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
UWB1.289 300 nmol/L 14 days To evaluate the effect of KSQ-4279 on DNA repair pathways in UWB1.289 cells, results showed that PARP1 knockout sensitized cells to KSQ-4279. Cancer Res. 2024 Oct 15;84(20):3419-3434
USP1-UAF1 enzyme 0.01 μM 20 minutes Evaluate the inhibitory effect of KSQ-4279 on USP1-UAF1 enzyme, showing almost complete inhibition of FANCI-FANCD2Ub deubiquitination in the presence of 25 μM KSQ-4279. J Med Chem. 2024 Sep 12;67(17):15557-15568
CAOV3 300 nmol/L 14 days To evaluate the effect of KSQ-4279 on clonogenic growth in CAOV3 cells, results showed that PCNA(K164R) mutation rendered cells insensitive to KSQ-4279. Cancer Res. 2024 Oct 15;84(20):3419-3434
MDA-MB-436 300 nmol/L 7 days To evaluate the effect of KSQ-4279 on apoptosis in MDA-MB-436 cells, results showed that KSQ-4279 treatment led to an increase in cleaved caspase-3, indicating induction of apoptosis. Cancer Res. 2024 Oct 15;84(20):3419-3434

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c nude or Athymic Nude-Foxn1nu mice OV0589 ovarian PDX model Oral gavage 10-300 mg/kg Once daily for 10 weeks To evaluate the antitumor activity of KSQ-4279 in the OV0589 model, results showed clear antitumor activity at 100 and 300 mg/kg doses with tumor regression observed. Cancer Res. 2024 Oct 15;84(20):3419-3434

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.87mL

0.37mL

0.19mL

9.35mL

1.87mL

0.94mL

18.71mL

3.74mL

1.87mL

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
 

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