For research use only. Not for therapeutic Use.
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 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].
| Catalog Number | I001673 |
| CAS Number | 1432908-05-8 |
| Synonyms | 6-[2-chloro-4-(6-methylpyrazin-2-yl)phenyl]-8-ethyl-2-[2-(1-methylpiperidin-4-yl)ethylamino]pyrido[2,3-d]pyrimidin-7-one |
| Molecular Formula | C28H32ClN7O |
| Purity | ≥95% |
| InChI | InChI=1S/C28H32ClN7O/c1-4-36-26-21(16-32-28(34-26)31-10-7-19-8-11-35(3)12-9-19)13-23(27(36)37)22-6-5-20(14-24(22)29)25-17-30-15-18(2)33-25/h5-6,13-17,19H,4,7-12H2,1-3H3,(H,31,32,34) |
| InChIKey | RYCBSFIKWACFBY-UHFFFAOYSA-N |
| SMILES | CCN1C2=NC(=NC=C2C=C(C1=O)C3=C(C=C(C=C3)C4=NC(=CN=C4)C)Cl)NCCC5CCN(CC5)C |
| Reference | [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. |
