FRAX597

SKU: orb1223352

Description

FRAX597 is a potent and selective inhibitor of the p21-activated kinases. FRAX597 inhibits tumorigenesis of neurofibromatosis type 2 (NF2)-associated Schwannomas. FRAX597 inhibits the proliferation of NF2-deficient schwannoma cells in culture and displayed potent anti-tumor activity in vivo, impairing schwannoma development in an orthotopic model of NF2. These studies identify a novel class of orally available ATP-competitive Group I PAK inhibitors with significant potential for the treatment of NF2 and other cancers.

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Key Properties

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CAS Number	1286739-19-2
MW	558.1
Purity	>98% (HPLC)
Formula	C₂₉H₂₈ClN₇OS
SMILES	CCn1c2nc(ncc2cc(c1=O)c1c(cc(cc1)c1cncs1)Cl)Nc1ccc(cc1)N1CCN(CC1)C
Target	EGFR
Solubility	DMSO : 14.29 mg/mL. 25.60 mM;H2O : < 0.1 mg/mL

Bioactivity

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In Vivo

Analysis of the flux reading for the animals in the two cohorts demonstrates a significantly slower tumor growth rate in FRAX597-treated mice compared with control mice. After 14 days of treatment the animals are sacrificed and the tumors excised and weighed. FRAX597-treated cohort shows significantly lower average tumor weight compared with the control cohort.

In Vitro

FRAX597 is determined to be a potent, ATP-competitive inhibitor of group I PAKs (PAK 1-3), with biochemical IC50 values as follows: PAK1 IC50 = 8 nM, PAK2 IC50 = 13 nM, PAK3 IC50 = 19 nM. The IC50 toward PAK4, a member of group II PAKs is >10 μM. At a concentration of 100 nM FRAX597 displays a significant (> 80% inhibition) inhibitory capacity toward YES1 (87%), RET (82%), CSF1R (91%), TEK (87%), PAK1 (82%), and PAK2 (93%). When measured using the Kinase Glo Assay in the presence of 20 nM protein and 1 μM ATP, FRAX597 displayed an IC50 value of 48 nM against wild type PAK1, while IC50 values against the V342F and V342Y PAK1 mutants are higher than 3 μM and 2 μM, respectively.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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FRAX597 | FRAX-597 | FRAX 597

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EGFR

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FRAX597 (orb1223352)

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Purity:	99.94% (May vary between batches)
CAS Number:	1286739-19-2
MW:	558.1
Formula:	C₂₉H₂₈ClN₇OS

FRAX597

Description

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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FRAX597 (orb1223352)

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