PAK4-IN-1
PAK4-IN-1 is an orally active PAK4 inhibitor. PAK4-IN-1 is hydrolyzed in rat plasma and liver S9 to the active parent CZh-226 (HY-111103), thereby increasing parent drug exposure, and shows antitumor efficacy in mouse tumor models. PAK4-IN-1 can be used for research on colon cancer and melanoma.
For research use only. We do not sell to patients.
- CAS No.: 2396529-58-9
- Formula: C26H30ClN7O5
- Molecular Weight:556.01
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
PAK4 |
In Vitro
PAK4-IN-1 (10-20 mM; 2 h) is stable in PBS and SGF, but less stable in SIF, with 93.5%, 90.0%, and 46.0% remaining after 2 h, respectively[1].
PAK4-IN-1 (20 µM; 2 h) rapidly hydrolyzes in rat plasma, with 6.1% remaining after 2 h and 89.9% converted to the parent compound 3[1].
PAK4-IN-1 (10 µM; 60 min) is extensively converted to the parent compound 3 in rat liver S9 fraction, with 14.0% remaining after 1 h and a conversion rate of 64.2%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
In Vivo
PAK4-IN-1 (25-50 mg/kg/d; p.o. (oral gavage); once daily; for 21 consecutive days) reduces B16F10 tumor volume by 51% and 63%, respectively, relative to the control[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BABL/c nude[1]
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Dosage:25 mg/kg/d; 50 mg/kg/d
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Administration:p.o. (oral gavage); once daily; 21 consecutive days
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Result:Tumor inhibition rates were 54% at 25 mg/kg/d and 65% at 50 mg/kg/d.
No mortality and no significant body weight loss (< 5% relative to vehicle-matched controls) were observed during the study.
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Animal Model:C57BL/6[1]
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Dosage:25 mg/kg/d; 50 mg/kg/d
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Administration:p.o. (oral gavage); once daily; 21 consecutive days
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Result:At the end of the experiment, average tumor volume in mice decreased by 51% at 25 mg/kg/d and 63% at 50 mg/kg/d relative to control groups.
No mortality and no significant body weight loss (< 5% relative to vehicle-matched controls) were observed during the study.
Chemical Information
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CAS No. 2396529-58-9
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Molecular Weight 556.01
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Formula C26H30ClN7O5
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SMILES
O=C(OCOC(C(C)C)=O)N1[C@@H](CN(CC1)C(C2=NC(NC3=NNC(C4CC4)=C3)=C5C=C(C=CC5=N2)Cl)=O)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PAK4-IN-1 Related Classifications
HY-130628 Related Classifications
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