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United States

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製品番号: HY-146210

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EGFR-IN-50

EGFR-IN-50 (Compound 9h) is a potent EGFR inhibitor against L858R resistance mutation (TEL-EGFR-L858R-BaF3: GI₅₀=8 nM, TEL-EGFR-T790M-L858R-BaF3: GI₅₀=6.03 μM). EGFR-IN-50 shows anti-proliferative activity to cancer cells.

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CAS 番号: 2044508-48-5
分子式: C₂₄H₂₆BrN₃O₄S₂
分子量:564.51

保管条件:

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

Data Sheet (268 KB)

EGFR-IN-50 構造式

CAS 番号: 2044508-48-5

価格（税別）

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Use of MCE Products

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

生物活性

製品説明

EGFR アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
HUVEC	IC₅₀	>10 μM Compound: 9h	Cytotoxicity against HUVEC assessed as reduction in cell viability measured after 72 hrs by Celltiter-Glo luminescent cell viability assay Cytotoxicity against HUVEC assessed as reduction in cell viability measured after 72 hrs by Celltiter-Glo luminescent cell viability assay	[PMID: 32619886]

体外実験

EGFR-IN-50 (0-10 μM; 72 h) selectively inhibits NSCLC cell line H3255 (expressing EGFR-L858R) compared to other tumor cells^[1].
EGFR-IN-50 (1-10 μM; 72 h) induces cell cycle arrest in G0-G1 phase^[1].
EGFR-IN-50 (0.039-10 μM; 4 h) inhibits the phosphorylation of EGFR in H3255 cells^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

A549, H3255, HepG2, MCF-7, HT-29 and A431 cells
Concentration:

0-10 μM
Incubation Time:

72 hours
Result:

Showed GI₅₀ values of >10, and 0.7873 μM for A549 and H3255 cells, respectively.
Showed IC₅₀ values of >10, 7.309, >10 and 6.703 μM for HepG2, MCF-7, HT-29 and A431 cells, respectively.

Cell Cycle Analysis^[1]

Cell Line:

H3255 cells
Concentration:

1, 5, and 10 μM
Incubation Time:

72 hours
Result:

Increased the percentage of H3255 cells in G0-G1 phase from 60.32% to 88.61%.

Western Blot Analysis^[1]

Cell Line:

H3255 cells
Concentration:

0.039, 0.15, 0.62, 2.5, and 10 μM
Incubation Time:

4 hours
Result:

Inhibited the phosphorylation of EGFR in H3255 cells in a dose-dependent manner.

化学情報

CAS 番号 2044508-48-5
分子量 564.51
分子式 C₂₄H₂₆BrN₃O₄S₂
SMILES

C=CCSSCCC(OCCCOC1=CC2=C(C(NC3=CC(Br)=CC=C3)=NC=N2)C=C1OC)=O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (268 KB)
COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[1]. You-Guang Zheng, et al. Design, synthesis and biological evaluation of 4-aniline quinazoline derivatives conjugated with hydrogen sulfide (H2S) donors as potent EGFR inhibitors against L858R resistance mutation. Eur J Med Chem. 2020 Sep 15;202:112522. [Content Brief]

Calculators

モル濃度計算機

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

Mass Mass

濃度濃度

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分子量分子量

希釈計算機

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濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

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.

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MOQ

Minimum order quantity

100 mg

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