1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  2. EGFR
  3. JBJ-09-063

JBJ-09-063 is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 can be used for researching EGFR-mutant lung cancer.

The free form of the compound is prone to instability, it is advisable to consider the stable salt form that retains the same biological activity.

For research use only. We do not sell to patients.

JBJ-09-063 Chemical Structure

JBJ-09-063 Chemical Structure

CAS No. : 2820336-67-0

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Description

JBJ-09-063 is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 can be used for researching EGFR-mutant lung cancer[1].

IC50 & Target[1]

EGFR L858R

0.147 nM (IC50)

EGFR L858R/T790M

0.063 nM (IC50)

EGFR L858R/T790M/C797S

0.083 nM (IC50)

EGFRLT/L747S

0.396 nM (IC50)

In Vitro

JBJ-09-063 is remarkably effective at inhibiting cell growth and leads to a significant increase in apoptosis, even though H3255GR cells are resistant to gefitinib as a single agent, as they contain an EGFR T790M mutation[1].
JBJ-09-063 is effective in H1975 cells exogenously expressing the osimertinib-resistant mutations[1].
JBJ-09-063 exhibits IC50s of 50 nM and 6 nM in Ba/F3 cell when use alone or combination with Cetuximab (HY-P9905)[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

JBJ-09-063 (3 mg/kg i.v., 20 mg/kg p.o.) exhibits favorable pharmacokinetics properties and is sufficiently stable to deliver good efficacy upon oral dosing[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Mice[2]
Dosage: 3 mg/kg for i.v., 20 mg/kg for p.o.
Administration: i.v. and p.o.; single dosage
Result: Pharmacokinetic Parameters of JBJ-09-063 in mice[2].
Cl (mL/min/kg), i.v. T1/2 (h) Vss (L/kg) F (%) AUC 8h (ng·h/mL)
15.7 2.3 2.5 15 2398
Molecular Weight

556.65

Formula

C31H29FN4O3S

CAS No.
SMILES

O=C(NC1=NC=CS1)C(C2=CC(F)=CC=C2O)N(CC3=C4C=C(C5=CC=C(C6CCN(C)CC6)C=C5)C=C3)C4=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 120 mg/mL (215.58 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7965 mL 8.9823 mL 17.9646 mL
5 mM 0.3593 mL 1.7965 mL 3.5929 mL
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Purity & Documentation
References

Complete Stock Solution Preparation Table

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7965 mL 8.9823 mL 17.9646 mL 44.9115 mL
5 mM 0.3593 mL 1.7965 mL 3.5929 mL 8.9823 mL
10 mM 0.1796 mL 0.8982 mL 1.7965 mL 4.4912 mL
15 mM 0.1198 mL 0.5988 mL 1.1976 mL 2.9941 mL
20 mM 0.0898 mL 0.4491 mL 0.8982 mL 2.2456 mL
25 mM 0.0719 mL 0.3593 mL 0.7186 mL 1.7965 mL
30 mM 0.0599 mL 0.2994 mL 0.5988 mL 1.4971 mL
40 mM 0.0449 mL 0.2246 mL 0.4491 mL 1.1228 mL
50 mM 0.0359 mL 0.1796 mL 0.3593 mL 0.8982 mL
60 mM 0.0299 mL 0.1497 mL 0.2994 mL 0.7485 mL
80 mM 0.0225 mL 0.1123 mL 0.2246 mL 0.5614 mL
100 mM 0.0180 mL 0.0898 mL 0.1796 mL 0.4491 mL
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JBJ-09-063 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
JBJ-09-063
Cat. No.:
HY-147183
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