EGFR T790M/L858R-IN-2

Name: EGFR T790M/L858R-IN-2
Brand: MedChemExpress
SKU: HY-149824
Rating: 4.5 (1 reviews)

Cat. No.: HY-149824 Purity: 99.66%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

EGFRT790M/L858R-IN-2 is a potent and selective EGFRT790M/L858R inhibitor with IC₅₀ values of 3.5, 1290 nM for EGFRT790M/L858R, EGFR WT, respectively. EGFRT790M/L858R-IN-2 decreases the expression of p-EGFR, P-AKT, P-ERK1/2. EGFRT790M/L858R-IN-2 induces Apoptosis and cell cycle arrest in the G1 phase. EGFRT790M/L858R-IN-2 shows anti-cancer activity.

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

EGFR T790M/L858R-IN-2 Chemical Structure

Size	Price	Stock	Quantity
5 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 720	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 1430	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 2280	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 3650	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Based on 1 publication(s) in Google Scholar

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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

3.5 nM (IC₅₀)

EGFR (WT)

1290 nM (IC₅₀)

EGFR^T790M

6.7 nM (IC₅₀)

EGFR^L858R

2.1 nM (IC₅₀)

In Vitro

EGFRT790M/L858R-IN-2 (compound 28f) (0.1, 1, 10 µM; 4 h) decreases the expression of p-EGFR, P-AKT, P-ERK1/2 in a dose-dependent manner in H1975, HCC827 cells^[1].
EGFRT790M/L858R-IN-2 (0.1, 1, 10 µM; 48 h) induces apoptosis and cell cycle arrest in the G1 phase in H1975, HCC827 cells^[1].
EGFRT790M/L858R-IN-2 (0.1, 1, 10 µM; 14 days) inhibits colony formation and cell migration in a dose-dependent manner^[1].

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

Western Blot Analysis^[1]

Cell Line:	H1975, HCC827, A549, A431cells
Concentration:	0.1, 1, 10 µM
Incubation Time:	4 h
Result:	Decreased the expression of p-EGFR, P-AKT, P-ERK1/2 in a dose-dependent manner in H1975, HCC827 cells, showed a weak inhibitory effect on EGF-induced EGFR and AKT and ERK1/2 phosphorylation in A549 and A431 cells.

Apoptosis Analysis^[1]

Cell Line:	H1975, HCC827, A549, A431cells
Concentration:	0.1, 1, 10 µM
Incubation Time:	48 h
Result:	Significantly induced apoptosis of H1975 and HCC827 cells in a dose-dependent manner, exhibited weaker apoptosis-inducing ability than osimertinib in A549 and A431 cells, inducing only 14.80 and 17.93% apoptosis, respectively, at 10 μM.

Cell Cycle Analysis^[1]

Cell Line:	H1975, HCC827, A549, A431cells
Concentration:	0.1, 1, 10 µM
Incubation Time:	48 h
Result:	Induced cell cycle arrest in the G1 phase with the G0/G1 phase ratios approximately 80.5% for H1975 and approximately 81.1% for HCC827，approximately 63.8% for A549 and approximately 64.5% for A431 cells.

In Vivo

EGFRT790M/L858R-IN-2 (5, 10, 20 mg/kg; i.p.; daily) inhibits tumor growth in a dose-dependent manner^[1].
Pharmacokinetic Parameters of EGFRT790M/L858R-IN-2 in Male Sprague-Dawley rats^[1].

parameter	i.v. (1 mg/kg)
T_1/2 (h)	1.76 ± 0.65
C_max (ng/mL)	649.90 ± 54.71
AUC_0-t (h*ng/ml)	1036.86 ± 137.03
AUC_0–∞ (h ng/ml)	1048.74 ± 134.39
V_z (mL/kg)	2515.40 ± 1184.92
CL(mL/min/kg)	16.07 ± 2.06

Male Sprague-Dawley rats, 1 mg/kg iv^[1]

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

Animal Model:	6-8 weeks, BALB/c female nude mice(H1975 cell xenografts)^[1]
Dosage:	5, 10, 20 mg/kg
Administration:	I.p.; once per day
Result:	Inhibited tumor growth, both in volume and weight in a dose-dependent manner.

Molecular Weight

497.57

Formula

C₂₈H₂₈FN₇O

Appearance

Solid

Color

Light yellow to yellow

SMILES

C=CC(NC1=CC=CC(NC2=C3C=C(F)C=CC3=NC(NC4=CC=C(N5CCN(C)CC5)C=C4)=N2)=C1)=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

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (200.98 mM; Need ultrasonic; 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	2.0098 mL	10.0488 mL	20.0977 mL
5 mM	0.4020 mL	2.0098 mL	4.0195 mL
10 mM	0.2010 mL	1.0049 mL	2.0098 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.

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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

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.66%

Select Batch:

Data Sheet (278 KB) SDS (251 KB)

COA (247 KB) HNMR (311 KB) RP-HPLC (407 KB)

Handling Instructions (2659 KB)

References

[1]. Pei J, et al. Design, Synthesis, and Antitumor Activity of Potent and Selective EGFR L858R/T790M Inhibitors and Identification of a Combination Therapy to Overcome Acquired Resistance in Models of Non-small-cell Lung Cancer. J Med Chem. 2023 Apr 27;66(8):5719-5752. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.0098 mL	10.0488 mL	20.0977 mL	50.2442 mL
	5 mM	0.4020 mL	2.0098 mL	4.0195 mL	10.0488 mL
	10 mM	0.2010 mL	1.0049 mL	2.0098 mL	5.0244 mL
	15 mM	0.1340 mL	0.6699 mL	1.3398 mL	3.3496 mL
	20 mM	0.1005 mL	0.5024 mL	1.0049 mL	2.5122 mL
	25 mM	0.0804 mL	0.4020 mL	0.8039 mL	2.0098 mL
	30 mM	0.0670 mL	0.3350 mL	0.6699 mL	1.6748 mL
	40 mM	0.0502 mL	0.2512 mL	0.5024 mL	1.2561 mL
	50 mM	0.0402 mL	0.2010 mL	0.4020 mL	1.0049 mL
	60 mM	0.0335 mL	0.1675 mL	0.3350 mL	0.8374 mL
	80 mM	0.0251 mL	0.1256 mL	0.2512 mL	0.6281 mL
	100 mM	0.0201 mL	0.1005 mL	0.2010 mL	0.5024 mL