FRAX1036
Based on 5 publication(s) in Google Scholar
FRAX1036 is a PAK inhibitor with Kis of 23.3 nM, 72.4 nM, and 2.4 μM for PAK1, PAK2 and PAK4, respectively.
For research use only. We do not sell to patients.
- Purity : 98.27%
- CAS No.: 1432908-05-8
- Formula: C28H32ClN7O
- Molecular Weight:518.05
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) FRAX1036
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Biological Activity
Description
IC50 & Target
[1]|
PAK1 23.3 nM (Ki) |
PAK2 72.4 nM (Ki) |
PAK4 2.4 μM (Ki) |
In Vitro
FRAX1036 is a PAK inhibitor with Kis of 23.3 nM, 72.4 nM, and 2.4 μM for PAK1, PAK2 and PAK4, respectively. FRAX1036 (2.5 μM) incombination with docetaxel alters stathmin phosphorylation, induces the apoptotic marker cleaved PARP and increases kinetics of apoptosis in MDA-MB-175 and HCC2911 cells; also alters microtubule organization, mitosis and cell fate in U2OS cells. Moreover, FRAX1036 shows significantly effective inhibition on U2OS cells[1]. FRAX1036 (10 μM) affects the proliferation of non-small cell lung cancer (NSCLC) cells when added to KRAS prenylation inhibitors[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
Chemical Information
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CAS No. 1432908-05-8
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Appearance Solid
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Molecular Weight 518.05
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Formula C28H32ClN7O
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Color White to light yellow
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SMILES
O=C1C(C2=CC=C(C3=NC(C)=CN=C3)C=C2Cl)=CC4=CN=C(NCCC5CCN(C)CC5)N=C4N1CC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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PLoS One
Synergistic effect of PAK and Hippo pathway inhibitor combination in NF2-deficient Schwannoma. [Abstract]2024 Jul 31;19(7):e0305121. PMID: 39083549 -
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bioRxiv
Network analysis of α-synuclein pathology progression reveals p21-activated kinases as regulators of vulnerability. [Abstract]2024 Oct 22:2024.10.22.619411. PMID: 39484617 -
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Elife
p27Kip1 promotes invadopodia turnover and invasion through the regulation of the PAK1/Cortactin pathway. [Abstract]2017 Mar 13:6:e22207. PMID: 28287395
Solvent & Solubility
In Vitro:
DMSO : 5.3 mg/mL (10.23 mM; Need warming; 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 10 mg/mL (19.30 mM); Suspended solution; Need ultrasonic
Purity & Documentation
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Data Sheet (274 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[1]. Ong CC, et al. Small molecule inhibition of group I p21-activated kinases in breast cancer induces apoptosis and potentiates the activity of microtubule stabilizing agents. Breast Cancer Res. 2015 Apr 23;17:59. [Content Brief]
[2]. Mortazavi F, et al. Significance of KRAS/PAK1/Crk pathway in non-small cell lung cancer oncogenesis. BMC Cancer. 2015 May 9;15:381. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.9303 mL | 9.6516 mL | 19.3032 mL | 48.2579 mL |
| 5 mM | 0.3861 mL | 1.9303 mL | 3.8606 mL | 9.6516 mL | |
| 10 mM | 0.1930 mL | 0.9652 mL | 1.9303 mL | 4.8258 mL |
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