FRAX597
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 407181

CAS#: 1286739-19-2

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.


Chemical Structure

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FRAX597
CAS# 1286739-19-2

Theoretical Analysis

MedKoo Cat#: 407181
Name: FRAX597
CAS#: 1286739-19-2
Chemical Formula: C29H28ClN7OS
Exact Mass: 557.17646
Molecular Weight: 558.1
Elemental Analysis: C, 62.41; H, 5.06; Cl, 6.35; N, 17.57; O, 2.87; S, 5.74

Size Price Shipping out time Quantity
5mg USD 280 2 Weeks
10mg USD 460 2 Weeks
50mg USD 960 2 Weeks
100mg USD 1475 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2021-03-07. Prices are subject to change without notice.

FRAX597, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.

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

Handling Instructions:

Preparing Stock Solutions

The following data is based on the product molecular weight 558.1 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.

Select a batch to recalculate based on the batch molecular weight:
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

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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.