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Cat. No.: HY-135805A

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(Rac)-JBJ-04-125-02

(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.

CAS No.: 2140807-05-0
Formula: C₂₉H₂₆FN₅O₃S
Molecular Weight:543.61

Storage:

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

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

CAS No.: 2140807-05-0

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Use of MCE Products

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

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)

All EGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	0.021 μM Compound: 2; JBJ-04-125-02	Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell growth in presence of cetuximab Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell growth in presence of cetuximab	[PMID: 35378251]
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	0.61 μM Compound: 2; JBJ-04-125-02	Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell growth Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell growth	[PMID: 35378251]
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.

Chemical Information

CAS No. 2140807-05-0
Appearance Solid
Molecular Weight 543.61
Formula C₂₉H₂₆FN₅O₃S
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (269 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 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]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References

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(Rac)-JBJ-04-125-02

All EGFR Isoforms