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Epertinib (hydrochloride)

CAT: 0804-HY-107367A-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-107367A-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
Epertinib (S-22611) hydrochloride is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER4 and HER2, with IC50s of 1.48 nM, 2.49 nM and 7.15 nM, respectively. Epertinib hydrochloride shows potent antitumor activity[1][2]. Epertinib (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
CAS Number
2071195-74-7
Product Name Alternative
S-22611 (hydrochloride)
UNSPSC
12352005
Target
EGFR
Type
Reference compound
Related Pathways
JAK/STAT Signaling; Protein Tyrosine Kinase/RTK
Applications
Neuroscience-Neuromodulation
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/epertinib-hydrochloride.html
Concentration
10mM
Purity
98.15
Solubility
DMSO : 125 mg/mL (ultrasonic) |H2O : 33.33 mg/mL (ultrasonic)
Smiles
CC#C/C(C1=CC2=C(NC3=CC=C(OCC4=CC=CC(F)=C4)C(Cl)=C3)N=CN=C2C=C1)=N\OC[C@@H]5NCCOC5.Cl
Molecular Formula
C30H28Cl2FN5O3
Molecular Weight
596.48
References & Citations
[1]Tanaka Y, et al. Distribution analysis of epertinib in brain metastasis of HER2-positive breast cancer by imaging mass spectrometry and prospect for antitumor activity. Sci Rep. 2018 Jan 10;8 (1) :343.|[2]Tanaka H, et al. Preclinical antitumor activity of S-222611, an oral reversible tyrosine kinase inhibitor of epidermal growth factor receptor and human epidermal growth factor receptor 2. Cancer Sci. 2014 Aug;105 (8) :1040-8.
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, sealed storage, away from moisture)
Scientific Category
Reference compound1
Clinical Information
Phase 2
Isoform
EGFR/ErbB1/HER1; ErbB2/HER2; ErbB4/HER4

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