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MedKoo Cat#: 407181 | Name: FRAX597
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

FRAX597
FRAX597
CAS#1286739-19-2

Theoretical Analysis

MedKoo Cat#: 407181

Name: FRAX597

CAS#: 1286739-19-2

Chemical Formula: C29H28ClN7OS

Exact Mass: 557.1765

Molecular Weight: 558.10

Elemental Analysis: C, 62.41; H, 5.06; Cl, 6.35; N, 17.57; O, 2.87; S, 5.74

Price and Availability

Size Price Availability Quantity
10mg USD 350.00 2 Weeks
25mg USD 650.00 2 Weeks
50mg USD 950.00 2 Weeks
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Related CAS #
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Synonym
FRAX597; FRAX-597; FRAX 597.
IUPAC/Chemical Name
6-[2-chloro-4-(1,3-thiazol-5-yl)phenyl]-8-ethyl-2-[4-(4-methylpiperazin-1-yl)anilino]pyrido[2,3-d]pyrimidin-7-one
InChi Key
DHUJCQOUWQMVCG-UHFFFAOYSA-N
InChi Code
InChI=1S/C29H28ClN7OS/c1-3-37-27-20(14-24(28(37)38)23-9-4-19(15-25(23)30)26-17-31-18-39-26)16-32-29(34-27)33-21-5-7-22(8-6-21)36-12-10-35(2)11-13-36/h4-9,14-18H,3,10-13H2,1-2H3,(H,32,33,34)
SMILES Code
O=C1C(C2=CC=C(C3=CN=CS3)C=C2Cl)=CC4=CN=C(NC5=CC=C(N6CCN(C)CC6)C=C5)N=C4N1CC
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
FRAX597 is a potent group I p21-activated Kinases (PAKs) inhibitor with IC50 of 8, 13 and 19 nM for PAK1, 2 and 3.
In vitro activity:
FRAX597 inhibited proliferation in all pancreatic cancer cell lines in a dose-dependent manner (Fig. 4a), with IC50 values between 650 nM for BxPC-3 cells and 2.0 μM for PANC-1 cells (Table 2). Similarly, FRAX597 inhibited migration and invasion in all pancreatic cancer cell lines in a dose-dependent manner (Fig. 4b), with IC50 values between 105 nM for MiaPaCa-2 cells and 605 nM for Pan02 cells (Table 2). Reference: BMC Cancer. 2016; 16: 24. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4715347/
In vivo activity:
Analysis of the flux reading for the animals in the two cohorts demonstrated a significantly slower tumor growth rate in FRAX597-treated mice compared with control mice (Fig. 5B). After 14 days of treatment the animals were sacrificed and the tumors excised and weighed. FRAX597-treated cohort showed significantly lower average tumor weight compared with the control cohort (0.55gr versus 1.87gr, p = 0.0001). Reference: J Biol Chem. 2013 Oct 4; 288(40): 29105–29114. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3790009/
Solvent mg/mL mM
Solubility
DMSO 15.1 27.07
DMF 14.0 25.09
Ethanol 0.5 0.91
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 558.10 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Yeo D, He H, Patel O, Lowy AM, Baldwin GS, Nikfarjam M. FRAX597, a PAK1 inhibitor, synergistically reduces pancreatic cancer growth when combined with gemcitabine. BMC Cancer. 2016 Jan 16;16:24. doi: 10.1186/s12885-016-2057-z. PMID: 26774265; PMCID: PMC4715347. 2. Licciulli S, Maksimoska J, Zhou C, Troutman S, Kota S, Liu Q, Duron S, Campbell D, Chernoff J, Field J, Marmorstein R, Kissil JL. FRAX597, a small molecule inhibitor of the p21-activated kinases, inhibits tumorigenesis of neurofibromatosis type 2 (NF2)-associated Schwannomas. J Biol Chem. 2013 Oct 4;288(40):29105-14. doi: 10.1074/jbc.M113.510933. Epub 2013 Aug 19. PMID: 23960073; PMCID: PMC3790009.
In vitro protocol:
1. Yeo D, He H, Patel O, Lowy AM, Baldwin GS, Nikfarjam M. FRAX597, a PAK1 inhibitor, synergistically reduces pancreatic cancer growth when combined with gemcitabine. BMC Cancer. 2016 Jan 16;16:24. doi: 10.1186/s12885-016-2057-z. PMID: 26774265; PMCID: PMC4715347. 2. Licciulli S, Maksimoska J, Zhou C, Troutman S, Kota S, Liu Q, Duron S, Campbell D, Chernoff J, Field J, Marmorstein R, Kissil JL. FRAX597, a small molecule inhibitor of the p21-activated kinases, inhibits tumorigenesis of neurofibromatosis type 2 (NF2)-associated Schwannomas. J Biol Chem. 2013 Oct 4;288(40):29105-14. doi: 10.1074/jbc.M113.510933. Epub 2013 Aug 19. PMID: 23960073; PMCID: PMC3790009.
In vivo protocol:
1. Yeo D, He H, Patel O, Lowy AM, Baldwin GS, Nikfarjam M. FRAX597, a PAK1 inhibitor, synergistically reduces pancreatic cancer growth when combined with gemcitabine. BMC Cancer. 2016 Jan 16;16:24. doi: 10.1186/s12885-016-2057-z. PMID: 26774265; PMCID: PMC4715347. 2. Licciulli S, Maksimoska J, Zhou C, Troutman S, Kota S, Liu Q, Duron S, Campbell D, Chernoff J, Field J, Marmorstein R, Kissil JL. FRAX597, a small molecule inhibitor of the p21-activated kinases, inhibits tumorigenesis of neurofibromatosis type 2 (NF2)-associated Schwannomas. J Biol Chem. 2013 Oct 4;288(40):29105-14. doi: 10.1074/jbc.M113.510933. Epub 2013 Aug 19. PMID: 23960073; PMCID: PMC3790009.
1: Beauchamp RL, James MF, DeSouza PA, Wagh V, Zhao WN, Jordan JT, Stemmer-Rachamimov A, Plotkin SR, Gusella JF, Haggarty SJ, Ramesh V. A high-throughput kinome screen reveals serum/glucocorticoid-regulated kinase 1 as a therapeutic target for NF2-deficient meningiomas. Oncotarget. 2015 Jul 10;6(19):16981-97. PubMed PMID: 26219339. 2: Mortazavi F, Lu J, Phan R, Lewis M, Trinidad K, Aljilani A, Pezeshkpour G, Tamanoi F. Significance of KRAS/PAK1/Crk pathway in non-small cell lung cancer oncogenesis. BMC Cancer. 2015 May 9;15:381. doi: 10.1186/s12885-015-1360-4. PubMed PMID: 25956913; PubMed Central PMCID: PMC4477307. 3: Chow HY, Dong B, Duron SG, Campbell DA, Ong CC, Hoeflich KP, Chang LS, Welling DB, Yang ZJ, Chernoff J. Group I Paks as therapeutic targets in NF2-deficient meningioma. Oncotarget. 2015 Feb 10;6(4):1981-94. PubMed PMID: 25596744; PubMed Central PMCID: PMC4385830. 4: Licciulli S, Maksimoska J, Zhou C, Troutman S, Kota S, Liu Q, Duron S, Campbell D, Chernoff J, Field J, Marmorstein R, Kissil JL. FRAX597, a small molecule inhibitor of the p21-activated kinases, inhibits tumorigenesis of neurofibromatosis type 2 (NF2)-associated Schwannomas. J Biol Chem. 2013 Oct 4;288(40):29105-14. doi: 10.1074/jbc.M113.510933. Epub 2013 Aug 19. PubMed PMID: 23960073; PubMed Central PMCID: PMC3790009. 5: Chow HY, Jubb AM, Koch JN, Jaffer ZM, Stepanova D, Campbell DA, Duron SG, O'Farrell M, Cai KQ, Klein-Szanto AJ, Gutkind JS, Hoeflich KP, Chernoff J. p21-Activated kinase 1 is required for efficient tumor formation and progression in a Ras-mediated skin cancer model. Cancer Res. 2012 Nov 15;72(22):5966-75. doi: 10.1158/0008-5472.CAN-12-2246. Epub 2012 Sep 14. PubMed PMID: 22983922; PubMed Central PMCID: PMC3500416.

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RSU 1150

RSU 1150