CRT0066101 (dihydrochloride)

CRT0066101 dihydrochloride is a potent and orally active PKD inhibitor with IC50 values of 1 nM, 2.5 nM and 2 nM for PKD1, PKD2, and PKD3, respectively[1]. CRT0066101 dihydrochloride is also a potent PIM2 inhibitor with an IC50 of ~135.7 nM. CRT0066101 dihydrochloride exhibits anti-inflammatory activity in mice LPS (HY-D1056) -induced lung injury models, and has anticancer effects[1][2][3].

Product Specifications

CAS Number

[1883545-60-5]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; Pim; PKD

Type

Reference compound

Related Pathways

Apoptosis; JAK/STAT Signaling

Applications

Cancer-Kinase/protease

Field of Research

Cancer; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/CRT0066101_dihydrochloride.html

Purity

99.92

Solubility

DMSO : 11.36 mg/mL (ultrasonic; warming; heat to 60°C) |H2O : 50 mg/mL (ultrasonic)

Smiles

OC1=CC=C(C2=CN(C)N=C2)C=C1C3=NC=CC(NC[C@H](N)CC)=N3.[H]Cl.[H]Cl

Molecular Formula

C18H24Cl2N6O

Molecular Weight

411.33

Precautions

H302, H315, H319, H335

References & Citations

[1]Harikumar KB, et al. A novel small-molecule inhibitor of protein kinase D blocks pancreatic cancer growth in vitro and in vivo. Mol Cancer Ther. 2010 May;9 (5) :1136-46.|[2]Xi Chen, et al. Identification and assessment of new PIM2 inhibitors for treating hematologic cancers: A combined approach of energy-based virtual screening and machine learning evaluation. Arch Pharm (Weinheim) . 2024 Jan 23:e2300516.|[3]Cui B, et al., Small molecule inhibitor CRT0066101 inhibits cytokine storm syndrome in a mouse model of lung injury. Int Immunopharmacol. 2023 Jul;120:110240.