(Rac)-JBJ-04-125-02

Cat. No.: HY-135805A: Data Sheet
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(Rac)-JBJ-04-125-02 is the racemate of JBJ-04-125-02. JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor.

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

(Rac)-JBJ-04-125-02 Chemical Structure

CAS No. : 2140807-05-0

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Solution
10 mM * 1 mL in DMSO		Ask For Quote & Lead Time
Solid
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Other In-stock Forms of (Rac)-JBJ-04-125-02:

(Rac)-JBJ-04-125-02 acetate

Other Forms of (Rac)-JBJ-04-125-02:

(Rac)-JBJ-04-125-02 acetate In-stock
JBJ-04-125-02 Get quote

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View All EGFR Isoform Specific Products:

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

Biological Activity
Purity & Documentation
References
Customer Review

Description

(Rac)-JBJ-04-125-02 is the racemate of JBJ-04-125-02. JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor^[1].

IC₅₀ & Target^[1]

EGFR (L858R/T790M)

0.26 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	0.1 μM Compound: 2; JBJ-04-125-02	Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant after 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant after 72 hrs by MTS assay	[PMID: 36279692]
BaF3	IC₅₀	0.1 μM Compound: 6; JBJ-04-125-02	Antiproliferative activity against mouse BaF3 cells stably transfected with EGFR L858R/T790M/C797S (unknown origin) assessed as inhibition of cell proliferation incubated for 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells stably transfected with EGFR L858R/T790M/C797S (unknown origin) assessed as inhibition of cell proliferation incubated for 72 hrs by MTS assay	[PMID: 33243531]
BaF3	IC₅₀	1550 nM Compound: 6; JBJ-04-125-02	Cytotoxicity against mouse BaF3 cells harboring EGFR L858R/C797S mutant assessed as reduction in cell viability measured after 72 hrs by cell titre glo luminescence assay Cytotoxicity against mouse BaF3 cells harboring EGFR L858R/C797S mutant assessed as reduction in cell viability measured after 72 hrs by cell titre glo luminescence assay	[PMID: 36178776]
BaF3	IC₅₀	30 nM Compound: 6; JBJ-04-125-02	Cytotoxicity against mouse BaF3 cells expressing EGFR L858R/T790M/C797S mutant assessed as reduction in cell viability measured after 72 hrs by cell titre glo luminescence assay Cytotoxicity against mouse BaF3 cells expressing EGFR L858R/T790M/C797S mutant assessed as reduction in cell viability measured after 72 hrs by cell titre glo luminescence assay	[PMID: 36178776]
Sf9	IC₅₀	73.1 nM Compound: 2b; JBJ-04-125-02	Inhibition of human C-terminal His-tagged and N-terminal GST-tagged EGFR L858R/T790M/C797S triple mutant ( 668 to 1210 amino acids) expressed in baculovirus infected Sf9 insect cells using Poly(Glu,Tyr) 4:1 as substrate after 60 mins by ELISA Inhibition of human C-terminal His-tagged and N-terminal GST-tagged EGFR L858R/T790M/C797S triple mutant ( 668 to 1210 amino acids) expressed in baculovirus infected Sf9 insect cells using Poly(Glu,Tyr) 4:1 as substrate after 60 mins by ELISA	[PMID: 31298540]

In Vitro

JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC₅₀ of 0.26 nM for EGFR^L858R/T790M^[1].

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

Molecular Weight

543.61

Formula

C₂₉H₂₆FN₅O₃S

CAS No.

2140807-05-0

Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=NC=CS1)C(C2=CC(F)=CC=C2O)N(CC3=C4C=C(C5=CC=C(N6CCNCC6)C=C5)C=C3)C4=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Purity & Documentation

Data Sheet (269 KB) SDS (251 KB) Handling Instructions (2659 KB)

References

[1]. To C, et al. Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor. Cancer Discov. 2019 Jul;9(7):926-943. [Content Brief]

(Rac)-JBJ-04-125-02 Related Classifications

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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:

(Rac)-JBJ-04-125-022140807-05-0EGFREpidermal growth factor receptorErbB-1HER1Allostericanti-proliferationT790M-mutantanti-tumorracemateInhibitorinhibitorinhibit

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