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%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

EGFR T790M/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. EGFR T790M/L858R-IN-2 decreases the expression of p-EGFR, P-AKT, P-ERK1/2. EGFR T790M/L858R-IN-2 induces Apoptosis and cell cycle arrest in the G1 phase. EGFR T790M/L858R-IN-2 shows anti-cancer activity.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

EGFR T790M/L858R-IN-2 화학구조

CAS No. : 2955607-40-4

사이즈	재고	수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Solid
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
25 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
200 mg	견적 받기
500 mg	견적 받기

or 대량구매 문의

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 1 publication(s) in Google Scholar

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All EGFR Isoform Specific Products:

View All Isoforms

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

Biological Activity
순도&문서
References
고객리뷰

제품 설명

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)

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	2.486 μM Compound: 28f	Cytotoxicity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability measured after 72 hrs by MTT assay Cytotoxicity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 37042119]
A549	IC₅₀	4.02 μM Compound: 28f	Cytotoxicity against human A549 cells harboring wild type EGFR assessed as reduction in cell viability measured after 72 hrs by MTT assay Cytotoxicity against human A549 cells harboring wild type EGFR assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 37042119]
HCC827	IC₅₀	0.008 μM Compound: 28f	Antiproliferative activity against human HCC827 cells harboring EGFR exon del 19 mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells harboring EGFR exon del 19 mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 37042119]
NCI-H1975	IC₅₀	0.019 μM Compound: 28f	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 37042119]

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

EGFR T790M/L858R-IN-2 (5, 10, 20 mg/kg; i.p.; daily) inhibits tumor growth in a dose-dependent manner^[1].
Pharmacokinetic Parameters of EGFR T790M/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.

분자량

497.57

화학식

C₂₈H₂₈FN₇O

CAS No.

2955607-40-4

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

선적

Room temperature in continental US; may vary elsewhere.

보관

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

용액&용해도

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.

몰농도 계산기
농도 희석 계산기

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

순도&문서

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