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Cat. No.: HY-143445

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EGFR-IN-48

EGFR-IN-48 is a potent and orally active EGFR inhibitor with IC₅₀s of 0.193 nM, 0.251 nM, 10.4 nM for EGFR^d19/TM/CS, EGFR^LR/TM/CS, EGFR^WT, respectively. EGFR-IN-48 inhibits the proliferation of BaF3^{EGFR del19/T790M/C797S} and PC-9^{EGFR del19/T790M/C797S} cells with IC₅₀s of 1.526, 66.7 nM, respectively.

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

CAS No.: 2882851-77-4
Formula: C₃₅H₄₇BrN₉O₄PS
Molecular Weight:800.75

Storage:

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

Data Sheet (271 KB)

EGFR-IN-48 Chemical Structure

CAS No.: 2882851-77-4

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Antibody-Drug Conjugates

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

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

Biological Activity

Description

IC₅₀ & Target

EGFR^d19/TM/CS

0.193 nM (IC₅₀)

EGFR^LR/TM/CS

0.251 nM (IC₅₀)

EGFR^WT

10.4 nM (IC₅₀)

All EGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	1.526 nM Compound: 23	Antiproliferative activity against mouse BaF3 cells harboring del19/T790M/C797S mutant assessed as inhibition of cell proliferation Antiproliferative activity against mouse BaF3 cells harboring del19/T790M/C797S mutant assessed as inhibition of cell proliferation	[PMID: 35413415]
PC-9	IC₅₀	66.7 nM Compound: 23	Antiproliferative activity against human PC-9 cells harboring EGFR del19/T790M/C797S mutant assessed as inhibition of cell proliferation Antiproliferative activity against human PC-9 cells harboring EGFR del19/T790M/C797S mutant assessed as inhibition of cell proliferation	[PMID: 35413415]

In Vitro

EGFR-IN-48 (compound 23) (10 nM) shows anti-proliferative activities against BaF3^{EGFR del19/T790M/C797S} and PC-9^{EGFR del19/T790M/C797S} cells with IC₅₀s of 1.526, 66.7 nM, respectively^[1].
EGFR-IN-48 exhibits potent inhibitory activities against various clinically relevant EGFR mutants with IC₅₀s of 10.4, 3.1, 0.9, 0.1, 0.2, 0.3, 0.2 nM for EGFR^WT, EGFR^LR, EGFR^del19, EGFR^del19/TM, EGFR^LR/TM, EGFR^LR/TM/CS, EGFR^drl19/TM/CS, respectively^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

BaF3^{EGFR del19/T790M/C797S}, PC-9^{EGFR del19/T790M/C797S} cells
Concentration:

10 nM
Incubation Time:
Result:

Showed anti-proliferative activities against BaF3^{EGFR del19/T790M/C797S} and PC-9^{EGFR del19/T790M/C797S} cells with IC₅₀s of 1.526, 66.7 nM, respectively.

In Vivo

EGFR-IN-48 (2 mg/kg for i.v.; 10 mg/kg for o.p.) shows good oral bioavailability and high plasma exposure in CD-1 mouse^[1]. Pharmacokinetic Parameters of EGFR-IN-48 in CD-1 mouse^[1].

Route	Dose (mg/kg)	V_dss (L/kg)	T_1/2 (h)	CL (L/h/kg)	AUC_0-last (h*ng/mL)	C_max (ng/mL)	T_max (h)	F (%)
i.v.	2	0.7	3.3	2.4	13820.0
p.o.	10				33811.0	6600.0	0.5	48.9

CD-1 mouse; 2 mg/kg for i.v.; 10 mg/kg for o.p.^[1].

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

Animal Model:

CD-1 mouse^[1]
Dosage:
Administration:

2 mg/kg for i.v.; 10 mg/kg for o.p.
Result:

Showed good oral bioavailability and high plasma exposure.

Chemical Information

CAS No. 2882851-77-4
Molecular Weight 800.75
Formula C₃₅H₄₇BrN₉O₄PS
SMILES

CCC1=CC(NC2=NC=C(C(NC3=CC=C4N=CC=NC4=C3P(C)(C)=O)=N2)Br)=C(C=C1N5CCC(CC5)N6CCN(CC6)CCS(C)(=O)=O)OC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 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]. Fang H, et al. Design, synthesis and evaluation of the Brigatinib analogues as potent inhibitors against tertiary EGFR mutants (EGFRdel19/T790M/C797S and EGFRL858R/T790M/C797S). Bioorg Med Chem Lett. 2022; 9:128729. [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.

Keywords

100 mg

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

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EGFR-IN-48

All EGFR Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

EGFR-IN-48 Related Classifications

HY-143445 Related Classifications