Free shipping on all orders over $ 500

FRAX597

Cat. No. M5323
FRAX597 Structure
Size Price Availability Quantity
2mg USD 54  USD54 In stock
5mg USD 100  USD100 In stock
10mg USD 170  USD170 In stock
50mg USD 510  USD510 In stock
100mg USD 850  USD850 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

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 Nf2-/-SC4 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 KrasG12D mice, treatment with FRAX597 (90 mg/kg/day, p.o.) causes tumor regression and loss of Erk and Akt activity.

Chemical Information
Molecular Weight 558.10
Formula C29H28ClN7OS
CAS Number 1286739-19-2
Solubility (25°C) 14 mg/mL warmed in DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Yeo D, et al. BMC Cancer. FRAX597, a PAK1 inhibitor, synergistically reduces pancreatic cancer growth when combined with gemcitabine.

[2] Licciulli S, et al. J Biol Chem. FRAX597, a small molecule inhibitor of the p21-activated kinases, inhibits tumorigenesis of neurofibromatosis type 2 (NF2)-associated Schwannomas.

Related PAK Products
st-Ht31

st-Ht31 is a membrane-permeable peptide inhibitor of protein kinase A (PKA) anchoring.

AZA197

AZA197 is a selective small molecule inhibitor of Cdc42.AZA197 suppresses colon cancer cell proliferation, cell migration, invasion and increases apoptosis by down-regulating the PAK1 and ERK signaling pathways in vitro.

ZMF-23

ZMF-23 is a PAK1/HDAC6 dual inhibitor.

PF-3758309 dihydrochloride

PF-3758309 (PF-03758309) dihydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 dihydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation.

AZ13705339 hemihydrate 

AZ13705339 hemihydrate is a highly potent and selective PAK1 inhibitor with IC50s of 0.33 nM and 59 nM for PAK1 and pPAK1, respectively. AZ13705339 hemihydrate has binding affinities to PAK1 and PAK2, with Kds of 0.28 nM and 0.32 nM, respectively. AZ13705339 hemihydrate can be used in the research of cancers.

  Catalog
Abmole Inhibitor Catalog




Keywords: FRAX597 supplier, PAK, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.