AZ13705339
Based on 1 Customer Validation
AZ13705339 is a highly potent and selective PAK1 inhibitor with IC50s of 0.33 nM and 59 nM for PAK1 and pPAK1, respectively. AZ13705339 has binding affinities to PAK1 and PAK2, with Kds of 0.28 nM and 0.32 nM, respectively. AZ13705339 can be used in the research of cancers.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.57%
- No. CAS: 2016806-57-6
- Fòrmula: C33H36FN7O3S
- Peso molecular:629.75
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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PAK2 0.32 nM (Kd) |
PAK1 0.28 nM (Kd) |
PAK1 0.33 nM (IC50) |
pPAK1 59 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.06 μM
Compound: AZ137-05339
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Growth inhibition of human A549 cells
Growth inhibition of human A549 cells
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[PMID: 28814374] |
| MCF-10A | IC50 |
0.059 μM
Compound: 18
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Inhibition of PAK1 phosphorylation in human MCF10A cells
Inhibition of PAK1 phosphorylation in human MCF10A cells
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[PMID: 27994749] |
| Sf21 | IC50 |
31 nM
Compound: 18
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Inhibition of N-terminal his6-tagged recombinant full-length human LYN expressed in baculovirus infected Sf21 cells
Inhibition of N-terminal his6-tagged recombinant full-length human LYN expressed in baculovirus infected Sf21 cells
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[PMID: 27994749] |
| Sf21 | IC50 |
7 nM
Compound: 18
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Inhibition of C-terminal 6His-tagged recombinant full length human PKCtheta expressed in fall armyworm Sf21 cells
Inhibition of C-terminal 6His-tagged recombinant full length human PKCtheta expressed in fall armyworm Sf21 cells
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[PMID: 27994749] |
| Sf21 | IC50 |
93 nM
Compound: 18
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Inhibition of N-terminal His6-tagged recombinant human Src (1 to 530 residues) expressed in baculovirus infected sf21 cells
Inhibition of N-terminal His6-tagged recombinant human Src (1 to 530 residues) expressed in baculovirus infected sf21 cells
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[PMID: 27994749] |
AZ13705339 (1 μM) inhibits αIgM-controlled adhesion and not PMA-induced adhesion in Namalwa cells[2].
AZ13705339 (300 nM, 30 min) prevents Siglec-8 engagement-induced eosinophil death[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 2016806-57-6
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Appearance Solid
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Peso molecular 629.75
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Fòrmula C33H36FN7O3S
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Color White to off-white
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SMILES
N#CC1=CC=CC=C1CN(C2=NC(NC3=CC=C(N4CCN(C)CC4)C(S(=O)(CC)=O)=C3)=NC=C2F)C5=CC(CO)=CC=C5C
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 250 mg/mL (396.98 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. McCoull W, Hennessy EJ, Blades K, et al. Optimization of Highly Kinase Selective Bis-anilino Pyrimidine PAK1 Inhibitors. ACS Med Chem Lett. 2016;7(12):1118-1123. Published 2016 Sep 14. [Content Brief]
[2]. Martin F M de Rooij, et al. A loss-of-adhesion CRISPR-Cas9 screening platform to identify cell adhesion-regulatory proteins and signaling pathways. Nat Commun. 2022 Apr 19;13(1):2136. [Content Brief]
[3]. Daniela J Carroll, et al. Siglec-8 Signals Through a Non-Canonical Pathway to Cause Human Eosinophil Death In Vitro. Front Immunol. 2021 Oct 11;12:737988. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.5879 mL | 7.9397 mL | 15.8793 mL | 39.6983 mL |
| 5 mM | 0.3176 mL | 1.5879 mL | 3.1759 mL | 7.9397 mL | |
| 10 mM | 0.1588 mL | 0.7940 mL | 1.5879 mL | 3.9698 mL | |
| 15 mM | 0.1059 mL | 0.5293 mL | 1.0586 mL | 2.6466 mL | |
| 20 mM | 0.0794 mL | 0.3970 mL | 0.7940 mL | 1.9849 mL | |
| 25 mM | 0.0635 mL | 0.3176 mL | 0.6352 mL | 1.5879 mL | |
| 30 mM | 0.0529 mL | 0.2647 mL | 0.5293 mL | 1.3233 mL | |
| 40 mM | 0.0397 mL | 0.1985 mL | 0.3970 mL | 0.9925 mL | |
| 50 mM | 0.0318 mL | 0.1588 mL | 0.3176 mL | 0.7940 mL | |
| 60 mM | 0.0265 mL | 0.1323 mL | 0.2647 mL | 0.6616 mL | |
| 80 mM | 0.0198 mL | 0.0992 mL | 0.1985 mL | 0.4962 mL | |
| 100 mM | 0.0159 mL | 0.0794 mL | 0.1588 mL | 0.3970 mL |
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