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FRAX-1036

Chemical Structure : FRAX-1036

CAS No.: 1432908-05-8

FRAX-1036 (FRAX1036;FRAX 1036)

Catalog No.: PC-45644Not For Human Use, Lab Use Only.

FRAX1036 is a potent and selective inhibitor of group I PAKs (PAK1, Ki=23.3 nM; PAK2, Ki=72.4 nM).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

FRAX1036 is a potent and selective inhibitor of group I PAKs (PAK1, Ki=23.3 nM; PAK2, Ki=72.4 nM).
FRAX1036 displays weak affinity on PAK4 (Ki = 2.4 uM).
FRAX1036 inhibits phosphorylation of MEK1-S298 and CRAF-S338 at 2.5-5 uM in MDA-MB-175 cells.
FRAX1036 inhibits MPNST cell growth in vitro and dramatically decreases local and metastatic MPNST growth in animal models combined with PD0325901.

Physicochemical Properties

M.Wt 518.053
Formula C28H32ClN7O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: 5.3 mg/mL (Need warming)

Chemical Name/SMILES

Pyrido[2,3-d]pyrimidin-7(8H)-one, 6-[2-chloro-4-(6-methyl-2-pyrazinyl)phenyl]-8-ethyl-2-[[2-(1-methyl-4-piperidinyl)ethyl]amino]-

References

1. Ong CC, et al. Breast Cancer Res. 2015 Apr 23;17:59.

2. Mortazavi F, et al. BMC Cancer. 2015 May 9;15:381.

3. Semenova G, et al. Oncogene. 2017 May 22. doi: 10.1038/onc.2017.143.

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