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MedKoo Cat#: 462076 | Name: JCN037
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

JCN037 is a potent brain-penetrant EGFR tyrosine kinase inhibitor against malignant brain tumors. JCN037 displayed potent activity against EGFR amplified/mutant patient-derived cell cultures, significant BBB penetration (2:1 brain-to-plasma ratio), and superior efficacy in an EGFR-driven orthotopic glioblastoma xenograft model.

Chemical Structure

JCN037
JCN037
CAS#2305154-31-6

Theoretical Analysis

MedKoo Cat#: 462076

Name: JCN037

CAS#: 2305154-31-6

Chemical Formula: C16H11BrFN3O2

Exact Mass: 375.0019

Molecular Weight: 376.19

Elemental Analysis: C, 51.09; H, 2.95; Br, 21.24; F, 5.05; N, 11.17; O, 8.51

Price and Availability

Size Price Availability Quantity
50mg USD 750.00 2 Weeks
100mg USD 1,250.00 2 Weeks
200mg USD 1,850.00 2 Weeks
500mg USD 3,250.00 2 Weeks
1g USD 4,650.00 2 Weeks
2g USD 7,450.00 2 Weeks
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Related CAS #
No Data
Synonym
JCN-037; JCN037; JCN 037
IUPAC/Chemical Name
N-(3-bromo-2-fluorophenyl)-7,8-dihydro-[1,4]dioxino[2,3-g]quinazolin-4-amine
InChi Key
MTLUFWWVOINWEL-UHFFFAOYSA-N
InChi Code
InChI=1S/C16H11BrFN3O2/c17-10-2-1-3-11(15(10)18)21-16-9-6-13-14(23-5-4-22-13)7-12(9)19-8-20-16/h1-3,6-8H,4-5H2,(H,19,20,21)
SMILES Code
FC1=C(Br)C=CC=C1NC2=C3C=C(OCCO4)C4=CC3=NC=N2
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
JCN037 (JGK037) is non-covalent and BBB-penetrant EGFR tyrosine kinase inhibitor, with IC50 values of 2.49 nM, 3.95 nM, 4.48 nM for EGFR, p-wtEGFR and pEGFRvⅢ, respectively.
In vitro activity:
Together, these results indicate that 5 (JCN037) can potently inhibit the signaling and growth of EGFRvIII mutant and EGFR amplified primary GBM cells at levels on par with or better than that of both erlotinib and lapatinib. Reference: ACS Med Chem Lett. 2020 May 1;11(10):1799-1809. https://pubmed.ncbi.nlm.nih.gov/33062157/
In vivo activity:
Conversely, tumors from 5 (JCN037)-treated mice showed a significant decrease in EGFRvIII activity that was associated with reduced RAS-MAPK and PI3K-AKT-mTOR signaling (Figure 2B and C). These data support the hypothesis that the heightened BBB penetration of 5 would result in a greater capacity to inhibit EGFR signaling in an orthotopic GBM xenograft model. Reference: ACS Med Chem Lett. 2020 May 1;11(10):1799-1809. https://pubmed.ncbi.nlm.nih.gov/33062157/
Solvent mg/mL mM comments
Solubility
DMSO 250.0 664.57
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 376.19 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Tsang JE, Urner LM, Kim G, Chow K, Baufeld L, Faull K, Cloughesy TF, Clark PM, Jung ME, Nathanson DA. Development of a Potent Brain-Penetrant EGFR Tyrosine Kinase Inhibitor against Malignant Brain Tumors. ACS Med Chem Lett. 2020 May 1;11(10):1799-1809. doi: 10.1021/acsmedchemlett.9b00599. PMID: 33062157; PMCID: PMC7549123.
In vitro protocol:
1. Tsang JE, Urner LM, Kim G, Chow K, Baufeld L, Faull K, Cloughesy TF, Clark PM, Jung ME, Nathanson DA. Development of a Potent Brain-Penetrant EGFR Tyrosine Kinase Inhibitor against Malignant Brain Tumors. ACS Med Chem Lett. 2020 May 1;11(10):1799-1809. doi: 10.1021/acsmedchemlett.9b00599. PMID: 33062157; PMCID: PMC7549123.
In vivo protocol:
1. Tsang JE, Urner LM, Kim G, Chow K, Baufeld L, Faull K, Cloughesy TF, Clark PM, Jung ME, Nathanson DA. Development of a Potent Brain-Penetrant EGFR Tyrosine Kinase Inhibitor against Malignant Brain Tumors. ACS Med Chem Lett. 2020 May 1;11(10):1799-1809. doi: 10.1021/acsmedchemlett.9b00599. PMID: 33062157; PMCID: PMC7549123.
1: Jonathan E. Tsang, Lorenz M. Urner, Gyudong Kim, Kingsley Chow, Lynn Baufeld, Kym Faull, Timothy F. Cloughesy, Peter M. Clark, Michael E. Jung, and David A. Nathanson. Development of a Potent Brain-Penetrant EGFR Tyrosine Kinase Inhibitor against Malignant Brain Tumors. ACS Medicinal Chemistry Letters Article ASAP. DOI: 10.1021/acsmedchemlett.9b00599