EGFR-IN-47

Cat. No.: HY-143337 Purity: 96.01%: FAQs
Data Sheet SDS COA Handling Instructions

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EGFR-IN-47 is a potent and orally active EGFR^{L858R/T790M/C797S} inhibitor with an IC₅₀ of 0.01 μM. EGFR-IN-47 induces cell cycle attest and cell apoptosis. EGFR-IN-47 has the potential for the research of NSCLC.

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

EGFR-IN-47 Chemical Structure

CAS No. : 3034649-73-2

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

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

EGFR^{L858R/T790M/C797S}

0.07 μM (IC₅₀)

In Vitro

EGFR-IN-47 (compound 14aj) (72 h) shows anti-proliferative effects with IC₅₀s of 0.013 μM, 2.972 μM, 1.031 μM for PC-9 (EGFR^{L858R/T790M/C797S}), A432, A549 cells, respectively^[1].
EGFR-IN-47 (0.01, 0.05, 0.25, 1 μM; 24 h) induces cell cycle attest at the G0/G1-phase^[1].
EGFR-IN-47 (0.01, 0.05, 0.25 μM) induces cell deathvia apoptosis in a concentration-dependent manner^[1].
EGFR-IN-47 (0.01, 0.05, 0.25, 1 μM) inhibits phosphorylation of the EGFR downstream mediators^[1].

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

Cell Cytotoxicity Assay^[1]

Cell Line:	PC-9 (EGFR^{L858R/T790M/C797S}), A432, A549 cells
Concentration:
Incubation Time:	72 h
Result:	Showed anti-proliferative effects with IC₅₀s of 0.013 µM, 2.972 µM, 1.031 µM for PC-9 (EGFR^{L858R/T790M/C797S}), A432, A549 cells, respectively.

Cell Cycle Analysis^[1]

Cell Line:	PC-9 EGFR^{L858R/T790M/C797S} cells
Concentration:	0.01, 0.05, 0.25, 1 µM
Incubation Time:	24 h
Result:	Cells were arrest at the G0/G1-phase.

Apoptosis Analysis^[1]

Cell Line:	PC-9 EGFR^{L858R/T790M/C797S} cells
Concentration:	0.01, 0.05, 0.25 µM
Incubation Time:	24 h
Result:	Induced cell deathvia apoptosis in a concentration-dependent manner.

Western Blot Analysis^[1]

Cell Line:	PC-9 EGFR^{L858R/T790M/C797S} cells
Concentration:	0.01, 0.05, 0.25, 1 µM
Incubation Time:
Result:	Inhibited phosphorylation of the EGFR downstream mediators.

In Vivo

EGFR-IN-47 (10, 20, 40 mg/kg; i.g.) shows anti-tumor effect with low toxicity^[1].
EGFR-IN-47 (20 mg/kg for i.v.; 20 mg/kg for p.o.) shows an ideal oral bioavailability of 66.05%^[1].
Pharmacokinetic Parameters of JAK1/TYK2-IN-2 in Male Sprague-Dawley rats^[1].

parameter	iv (20 mg/kg)	po (20 mg/kg)
AUC_0-∞ (mg/Lh)	15.889	10.494
C_max (mg/L)	6.845	0.77
T_max (h)	0.083	6
F (%)		66.05
MRT_0-∞ (h)	16.439	16.791
V_ss (L/kg)	16.015	28.101
CL (L/h/kg)	1.272	2.151
t_(1/2) (h)	8.922	11.154

Male Sprague-Dawley rats; 20 mg/kg for i.v.; 20 mg/kg for p.o.^[1]

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

Animal Model:	6-8 weeks, BALB/c nude mice (PC-9 EGFR^{L858R/T790M/C797S} cells )^[1]
Dosage:	10, 20, 40 mg/kg (dissolved in 25% (v/v) PEG400 plus 5% DMSO)
Administration:	I.g.
Result:	Showed anti-tumor effect with low toxicity.

Animal Model:	Male Sprague-Dawley rats^[1]
Dosage:	20 mg/kg
Administration:	I.v.; p.o.
Result:	Showed an ideal oral bioavailability of 66.05%.

Molecular Weight

481.64

Formula

C₂₉H₃₅N₇

CAS No.

3034649-73-2

Appearance

Solid

Color

Light yellow to yellow

SMILES

CN(CC1)CCN1C2=CC=C(C=C2)NC3=NC=C4C=C(N(C4=N3)C5CCCC5)CNC6=CC=CC=C6

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 20 mg/mL (41.52 mM; ultrasonic and warming and heat to 60°C; 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	2.0762 mL	10.3812 mL	20.7624 mL
5 mM	0.4152 mL	2.0762 mL	4.1525 mL
10 mM	0.2076 mL	1.0381 mL	2.0762 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

Purity: 96.01%

Select Batch:

Data Sheet (282 KB) SDS (251 KB)

COA (253 KB) HNMR (266 KB) RP-HPLC (270 KB) MS (68 KB)

Handling Instructions (2659 KB)

References

[1]. Wang C, et al. Discovery and structural optimization of potent epidermal growth factor receptor (EGFR) inhibitors against L858R/T790M/C797S resistance mutation for lung cancer treatment. Eur J Med Chem. 2022; 237:114381. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.0762 mL	10.3812 mL	20.7624 mL	51.9060 mL
	5 mM	0.4152 mL	2.0762 mL	4.1525 mL	10.3812 mL
	10 mM	0.2076 mL	1.0381 mL	2.0762 mL	5.1906 mL
	15 mM	0.1384 mL	0.6921 mL	1.3842 mL	3.4604 mL
	20 mM	0.1038 mL	0.5191 mL	1.0381 mL	2.5953 mL
	25 mM	0.0830 mL	0.4152 mL	0.8305 mL	2.0762 mL
	30 mM	0.0692 mL	0.3460 mL	0.6921 mL	1.7302 mL
	40 mM	0.0519 mL	0.2595 mL	0.5191 mL	1.2976 mL

EGFR-IN-47 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:

EGFR-IN-473034649-73-2ApoptosisEGFREpidermal growth factor receptorErbB-1HER1Low toxicityanti-tumorapoptosisphosphorylationG0/G1-phase,orally activePC-9 EGFR^{L858R/T790M/C797S} cellsInhibitorinhibitorinhibit

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