[CAS NO. 1432908-05-8] FRAX1036
PRODUCTS SPECIFICATIONS [1432908-05-8]
DESCRIPTION [1432908-05-8]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 518.05 |
| Molecular Formula | C28H32ClN7O |
| SMILES | O=C1C(C2=CC=C(C3=NC(C)=CN=C3)C=C2Cl)=CC4=CN=C(NCCC5CCN(C)CC5)N=C4N1CC |
1 Publications Citing Use of MCE
Summary
IC50 & Target
|
PAK1 23.3 nM (Ki) |
PAK2 72.4 nM (Ki) |
PAK4 2.4 μM (Ki) |
In Vitro
FRAX1036 is a PAK inhibitor with K i s 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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 5.3 mg/mL ( 10.23 mM ; Need warming)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.9303 mL | 9.6516 mL | 19.3032 mL |
| 5 mM | 0.3861 mL | 1.9303 mL | 3.8606 mL |
| 10 mM | 0.1930 mL | 0.9652 mL | 1.9303 mL |
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.
- [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.