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Chemical Structure| 1643913-93-2 Chemical Structure| 1643913-93-2

Structure of Padnarsertib
CAS No.: 1643913-93-2

Chemical Structure| 1643913-93-2

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PAK4-IN-1 is an inhibitor of p21-activated kinases (PAKs), with IC50 of ≤100 nM in MTT assay.

Synonyms: KPT-9274; ATG-019

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Product Details of Padnarsertib

CAS No. :1643913-93-2
Formula : C35H29F3N4O3
M.W : 610.63
SMILES Code : O=C(NCC1=CC2=CC(C3=CC=C(C(N4CCC(F)(F)CC4)=O)C=C3)=CC(C5=CC=C(F)C=C5)=C2O1)/C=C/C6=CC=C(N)N=C6
Synonyms :
KPT-9274; ATG-019
MDL No. :MFCD30207881

Safety of Padnarsertib

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

Related Pathways of Padnarsertib

cytoskeleton

Isoform Comparison

Biological Activity

Description
Padnarsertib (KPT-9274) is an orally bioavailable inhibitor targeting both PAK4 and Nicotinamide phosphoribosyltransferase (Nampt), with IC50 values of <100 nM and 120 nM, respectively [1][2][3].

In Vitro:

Cell Line
Concentration Treated Time Description References
Hct116 cells 20 ×10^−6M 24 hours To evaluate the effect of terbinafine on CRC cell viability, results showed that terbinafine significantly reduced the viability of HCT116 cells. PMC9596822

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c nude mice Intracranial glioblastoma xenograft model Oral gavage 10 mg/kg To evaluate the inhibitory effect of Cobicistat (CYP3A5 inhibitor) on glioblastoma growth. Results showed that the combination of Cobicistat and TMZ significantly suppressed tumor growth and prolonged mouse survival. PMC11697892

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT04914845 Acute Myeloid Leukemia|Acute M... More >>yeloid Leukemia, in Relapse|Acute Myeloid Leukemia Refractory Less << PHASE1 RECRUITING 2027-02-08 UCHealth-Metro Denver, Aurora,... More >> Colorado, 80045, United States|University of Colorado Hospital, Aurora, Colorado, 80045, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.64mL

0.33mL

0.16mL

8.19mL

1.64mL

0.82mL

16.38mL

3.28mL

1.64mL

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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