AZ13705339 hemihydrate
Based on 1 Customer Validation
AZ13705339 hemihydrate is a highly potent and selective PAK1 inhibitor with IC50s of 0.33 nM and 59 nM for PAK1 and pPAK1, respectively. AZ13705339 hemihydrate has binding affinities to PAK1 and PAK2, with Kds of 0.28 nM and 0.32 nM, respectively. AZ13705339 hemihydrate can be used in the research of cancers.
For research use only. We do not sell to patients.
- Purity: 99.77%
- Formula: C33H36FN7O3S.1/2H2O
- Molecular Weight:638.77
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
|
PAK2 0.32 nM (Kd) |
PAK1 0.28 nM (Kd) |
PAK1 0.33 nM (IC50) |
pPAK1 59 nM (IC50) |
AZ13705339 (1 μM) hemihydrate 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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Appearance Solid
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Molecular Weight 638.77
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Formula C33H36FN7O3S.1/2H2O
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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.O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (156.55 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)
Purity & Documentation
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Data Sheet (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. McCoull W, 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 | 1.5655 mL | 7.8275 mL | 15.6551 mL | 39.1377 mL |
| 5 mM | 0.3131 mL | 1.5655 mL | 3.1310 mL | 7.8275 mL | |
| 10 mM | 0.1566 mL | 0.7828 mL | 1.5655 mL | 3.9138 mL | |
| 15 mM | 0.1044 mL | 0.5218 mL | 1.0437 mL | 2.6092 mL | |
| 20 mM | 0.0783 mL | 0.3914 mL | 0.7828 mL | 1.9569 mL | |
| 25 mM | 0.0626 mL | 0.3131 mL | 0.6262 mL | 1.5655 mL | |
| 30 mM | 0.0522 mL | 0.2609 mL | 0.5218 mL | 1.3046 mL | |
| 40 mM | 0.0391 mL | 0.1957 mL | 0.3914 mL | 0.9784 mL | |
| 50 mM | 0.0313 mL | 0.1566 mL | 0.3131 mL | 0.7828 mL | |
| 60 mM | 0.0261 mL | 0.1305 mL | 0.2609 mL | 0.6523 mL | |
| 80 mM | 0.0196 mL | 0.0978 mL | 0.1957 mL | 0.4892 mL | |
| 100 mM | 0.0157 mL | 0.0783 mL | 0.1566 mL | 0.3914 mL |