JBJ-09-063

Cat. No.: HY-147183: FAQs
Data Sheet Handling Instructions

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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

CAS No. : 2820336-67-0

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This product is a controlled substance and not for sale in your territory.

Other Forms of JBJ-09-063:

JBJ-09-063 TFA Get quote
JBJ-09-063 hydrochloride Get quote

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View All Isoforms

EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

Biological Activity
Purity & Documentation
References
Customer Review

Description

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.	T_1/2 (h)	V_ss (L/kg)	F (%)	AUC 8h (ng·h/mL)
15.7	2.3	2.5	15	2398

Molecular Weight

556.65

Formula

C₃₁H₂₉FN₄O₃S

CAS No.

2820336-67-0

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
10 mM	0.1796 mL	0.8982 mL	1.7965 mL

View the Complete Stock Solution Preparation Table

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. To C, et al. An allosteric inhibitor against the therapy-resistant mutant forms of EGFR in non-small cell lung cancer. Nat Cancer. 2022 Apr;3(4):402-417. [Content Brief]

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

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.

Keywords:

JBJ-09-0632820336-67-0EGFREpidermal growth factor receptorErbB-1HER1EGFR-mutantlung cancerTKI-sensitiveresistantH3255GRH1975Ba/F3AnticancerInhibitorinhibitorinhibit

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