FRAX1036

Catalog No.S7989 Batch:S798901

Print

Technical Data

Formula

C28H32ClN7O
Molecular Weight 518.05 CAS No. 1432908-05-8
Solubility (25°C)* In vitro 4-Methylpyridine 21 mg/mL warmed with 50ºC water bath (40.53 mM)
DMSO Insoluble
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description FRAX-1036 is a potent and selective PAK inhibitor with biochemical potency (Ki) of 23.3 nM and 72.4 nM against PAK1 and PAK2.
Targets
PAK1 [1]
(Cell-free assay)		 PAK2 [1]
(Cell-free assay)		 PAK4 [1]
(Cell-free assay)
23.3 nM(Ki) 72.4 nM(Ki) 2.4 μM(Ki)
In vitro Potent cellular inhibition of group I PAK substrate phosphorylation (MEK1-S298 and CRAF-S338) was observed at 2.5 to 5 μM concentrations of FRAX1036 in PAK1-amplified MDA-MB-175 cells. Treatment of PAK1-amplified breast cancer cells with FRAX1036 results in apoptosis[1]. And treatment of OVCAR-3 cells with FRAX-1036 results in upregulation of p53 and p21, while down-regulating cyclin B1[3].
In vivo Treatment with Frax1036 results in slower KT21 tumor growth and is unlikely to have significant blood brain barrier permeability in mice[4].

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    MDA-MB175 cells

  • Concentrations

    0, 0.5, 1, 2.5, 5 μM

  • Incubation Time

    24 h

  • Method

    MDA-MB175 cells are treated with increasing concentrations of FRAX1036 for 24 hours. Cell lysates are immunoblotted with antibodies against biomarkers involved in PAK1 effector and survival signaling.
Animal Study:

[2]
  • Animal Models

    Pak2-deficient mice

  • Dosages

    30 mg/kg

  • Administration

    by oral gavage

Selleck's FRAX1036 has been cited by 5 publications

Targetable leukemia dependency on noncanonical PI3Kγ signaling [ bioRxiv, 2023, 10.1101/2023.12.15.571909] PubMed: none
MICAL1 activation by PAK1 mediates actin filament disassembly [ Cell Rep, 2022, 41(1):111442] PubMed: 36198272
EGFR activation limits the response of liver cancer to lenvatinib [ Nature, 2021, 595(7869):730-734] PubMed: 34290403
Functional proteomics interrogation of the kinome identifies MRCKA as a therapeutic target in high-grade serous ovarian carcinoma. [ Sci Signal, 2020, 13(619)] PubMed: 32071169
ROCK1 but not LIMK1 or PAK2 is a key regulator of apoptotic membrane blebbing and cell disassembly. [ Cell Death Differ, 2019, 10.1038/s41418-019-0342-5] PubMed: 31043701

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.