[CAS NO. 1286739-19-2] FRAX597
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PRODUCTS SPECIFICATIONS [1286739-19-2]
Store
Catalog
SLK-S7271
Brand
Selleck
CAS
1286739-19-2
DESCRIPTION [1286739-19-2]
Overview
| MDL | MFCD25976723 |
|---|---|
| Molecular Weight | 558.10 |
| Molecular Formula | C29H28ClN7OS |
| SMILES | O=C1C(C2=CC=C(C3=CN=CS3)C=C2Cl)=CC4=CN=C(NC5=CC=C(N6CCN(C)CC6)C=C5)N=C4N1CC |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7918 mL | 8.9590 mL | 17.9179 mL |
| 5 mM | 0.3584 mL | 1.7918 mL | 3.5836 mL |
| 10 mM | - | - | - |
| 50 mM | - | - | - |
Description
FRAX597 is a potent, ATP-competitive inhibitor of group I with of 8 nM, 13 nM, and 19 nM for PAK1, PAK2, and PAK3, respectively.
In vitro
FRAX597 (100 n M) displays a significant inhibitory capacity toward YES1 (87%), RET (82%), CSF1R (91%), TEK (87%), PAK1 (82%), and PAK2 (93%), while displays minimal inhibitory activity towards the group II PAKs: PAK4 (0%), PAK6 (23%), and PAK7 (8%). FRAX597 treatment dramatically impairs the proliferation of Nf2-null SC4 Schwann cells (SC4 cells). FRAX597 displays an IC50 value of 48 nM against wild type PAK1, while IC 50 values against the V342F and V342Y PAK1 mutants are higher than 3μM and 2 μM, respectively. FRAX597 inhibits the proliferation and motility of both benign (Ben-Men1, 3μM) and malignant (KT21-MG1, 0.4 μM) meningiomas cells after treating of 72 h.
In vivo
In NOD/SCID mice which bearing Nf2SC4 Schwann cells, FRAX597 (100 mg/kg/day, p.o.) causes more significant tumor growth inhibition cpmpared with control mice. In SCID mice with orthotopic meningioma, FRAX597 (90 mg/kg/day, p.o.) significantly suppresses tumor growth. In Kras mice, treatment with FRAX597 (90 mg/kg/day, p.o.) causes tumor regression and loss of Erk and Akt activity.
References
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