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CRT0066101

CAT: 0804-HY-15698-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-15698-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
CRT0066101 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 is also a potent PIM2 inhibitor with an IC50 of ~135.7 nM. CRT0066101 exhibits anti-inflammatory activity in mice LPS -induced lung injury models, and has anticancer effects[1][2][3].
CAS Number
956123-34-5
UNSPSC
12352005
Hazard Statement
H302, H312, H332
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.html
Purity
99.88
Solubility
DMSO : 100 mg/mL (ultrasonic)
Smiles
N[C@H](CC)CNC1=NC(C2=C(O)C=CC(C3=CN(C)N=C3)=C2)=NC=C1
Molecular Formula
C18H22N6O
Molecular Weight
338.41
Precautions
H302, H312, H332
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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 1
Isoform
PIM2; PKD1; PKD2; PKD3