Zelasudil

Zelasudil (RXC007) is an orally active, highly selective small molecule Rho-associated coiled-coil containing protein kinase 2 (ROCK2) inhibitor with anti-fibrotic efficacy. Zelasudil elicits positive immunomodulatory effects in metastatic pancreatic tumors with increase of CD8+ and CD4+ T cell infiltrate into the tumor cortex and reduction in immunosuppressive FOXP3+ regulatory T cells at the tumor border. Zelasudil is promising for research of pancreatic ductal adenocarcinoma[1][2][3][4].

Product Specifications

CAS Number

[2365193-22-0]

Product Name Alternative

RXC007

UNSPSC

12352005

Target

ROCK

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Cytoskeleton; Stem Cell/Wnt; TGF-beta/Smad

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/zelasudil.html

Purity

99.33

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(C1=CC=C(C2=NN(C)C(NC3=CC=C4NN=CC4=C3C5CC5)=N2)C=C1)NCC(F)F

Molecular Formula

C22H21F2N7O

Molecular Weight

437.45

References & Citations

[1]Lee E, et al. Selective ROCK2 inhibition for treatment of edema and associated conditions: World Intellectual Property Organization, WO2022169946. 2022-08-11.|[2]WHO Drug Information-World Health Organization (WHO) .|[3]Pajic M, et al. Combining zelasudil, a small molecule ROCK2 inhibitor, with chemotherapy or immunotherapy improves response in preclinical models of pancreatic cancer[J]. Cancer Research, 2024, 84 (6_Supplement) : 720-720.|[4]Gambardella A, et al. Effects of RXC007, a highly potent and selective ROCK2 inhibitor, in ex-vivo and in vivo models of pulmonary fibrosis[C]//European Respiratory Journal. 442 GLOSSOP RD, SHEFFIELD S10 2PX, ENGLAND: EUROPEAN RESPIRATORY SOC JOURNALS LTD, 2022, 60.