CH5138303

CH5138303 is a potent and orally active Hsp90 inhibitor. CH5138303 shows high binding affinity for N-terminal Hsp90α, with Kd of 0.52 nM. CH5138303 shows potent anti-proliferative activity against human cancer cell lines (HCT116 and NCI-N87), with IC50 values of 0.098 and 0.066 μM, respectively. CH5138303 shows high oral bioavailability in mice (F=44.0%) . CH5138303 shows potent antitumor efficacy in a human NCI-N87 gastric cancer xenograft model[1][2].

Product Specifications

CAS Number

[959763-06-5]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

HSP

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Metabolic Enzyme/Protease

Applications

COVID-19-anti-virus

Field of Research

Cancer; Infection

Assay Protocol

https://www.medchemexpress.com/ch5138303.html

Purity

99.05

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(N)CCCSC1=NC(N)=NC(C2=C(Cl)C=C3C4=C2C=CC=C4COC3)=N1

Molecular Formula

C19H18ClN5O2S

Molecular Weight

415.90

Precautions

H302, H315, H319, H335

References & Citations

[1]Atsushi Suda, et al. Design and synthesis of 2-amino-6- (1H,3H-benzo[de]isochromen-6-yl) -1,3,5-triazines as novel Hsp90 inhibitors. Bioorganic & Medicinal Chemistry. 15 January 2014;22 (2) :892-905.|[2]Yuan R, et al. Effects of Hsp90 Inhibitor Ganetespib on Inhibition of Azole-Resistant Candida albicans. Front Microbiol. 2021 May 20;12:680382.