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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.

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CAS No.: 2882851-77-4
Formule: C₃₅H₄₇BrN₉O₄PS
Masse moléculaire:800.75

Stockage:

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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Amount: USD 0.00

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Use of MCE Products

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

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Protocole (1)
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

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)

Voir tous les produits spécifiques à Isoform EGFR :

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. Further protocols information, click here.

Cell Proliferation Assay^[1]

View Protocol

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
Masse moléculaire 800.75
Formule 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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Protocole

All Cell Biology

Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (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)
Instruction de manipulation (2659 KB)

Références

[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

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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