製品番号: HY-164718

Sevabertinib

(別名: BAY 2927088)

カスタマーレビュー

Based on 1 Customer Validation

Sevabertinib (BAY 2927088) is an orally active and reversible dual EGFR-HER2 inhibitor (IC⁵⁰ <0.5 nM for wild-type HER2, HER2 A775insYVMA, wild-type EGFR, and EGFR D770_N771insSVD). Sevabertinib has anticancer activity against lung cancer.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度: 99.90%
CAS 番号: 2521285-05-0
分子式: C₂₄H₂₅ClN₄O₅
分子量:484.93

保管条件:

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

Sevabertinib 構造式

CAS 番号: 2521285-05-0

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Top Publications Citing

Use of MCE Products

Antibody-Drug Conjugates

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

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
- 臨床実験
化学情報
溶剤 & 溶解度
- 体外
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

IC⁵⁰: <0.5 nM for wild-type HER2, HER2 A775insYVMA, wild-type EGFR, and EGFR D770_N771insSVD^[2]

EGFR アイソフォーム固有の製品をすべて表示 :

体外実験

Sevabertinib exhibits an IC⁵⁰ of <0.5 nM against wild-type HER2, HER2 A775insYVMA, wild-type EGFR, and EGFR D770_N771insSVD at a physiological ATP concentration of 2 mM, and shows significantly reduced activity against HER4 (IC⁵⁰ = 13.9 nM)^[2].
Sevabertinib potently inhibits the proliferation of isogenic Ba/F3 cells ectopically expressing HER2 exon 20 insertions, activating HER2 point mutations, or putative secondary acquired resistance mutations (T798M, T798I, C805S)^[2].
Sevabertinib potently inhibits the proliferation of two lung cancer cell lines: NCI-H1781 (harboring HER2 exon 20 insertion mutations A775insV and G776C) with an IC⁵⁰ of 19.7 nM, and NCI-H2170 (harboring wild-type ERBB2 amplification) with an IC⁵⁰ of 16.7 nM^[2].

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

体内実験

Sevabertinib (10-50 mg/kg; p.o.; once daily) inhibits tumor growth and reduces tumor weight in the subcutaneous CTG-2543 PDX mouse model of NSCLC^[2].
Sevabertinib (5-10 mg/kg; p.o.; twice daily for 5 mg/kg; once daily for 10 mg/kg) demonstrates antitumor efficacy in the NCI-H1781 xenograft mouse model, with similar efficacy to Zongertinib (HY-148810)^[2].

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

Animal Model:

Nude mice + subcutaneous CTG-2543 PDX NSCLC model (HER2 A775insYVMA)^[2]
Dosage:

10 mg/kg, 25 mg/kg, 50 mg/kg
Administration:

Oral gavage, once daily (QD)
Result:

Showed T/C ratios of 0.22, 0.12, and 0.06 at doses of 10 mg/kg, 25 mg/kg, and 50 mg/kg, respectively.
Was well-tolerated as no marked body weight loss was observed.

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 2521285-05-0
性状 Solid
分子量 484.93
分子式 C₂₄H₂₅ClN₄O₅
Color Light yellow to yellow
SMILES

O=C(NCC1)C2=C1NC(C3=CC=NC=C3OC[C@@H]4COCCO4)=C2NC5=C(C(Cl)=CC=C5)OC
別名

BAY 2927088
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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

溶剤 & 溶解度

体外:

DMSO : 50 mg/mL (103.11 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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0622 mL

10.3108 mL

20.6215 mL

5 mM

0.4124 mL

2.0622 mL

4.1243 mL

10 mM

0.2062 mL

1.0311 mL

2.0622 mL

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.

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

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)

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 (278 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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]. International Nonproprietary Names for Pharmaceutical Substances (INN). WHO Drug Information, Vol. 38, No. 2, 2024.

[2]. Siegel F, et al. Sevabertinib, a Reversible HER2 Inhibitor with Activity in Lung Cancer. Cancer Discov. 2025 Oct 15. [Content Brief]

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.

Complete Stock Solution Preparation Table

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.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0622 mL	10.3108 mL	20.6215 mL	51.5538 mL
	5 mM	0.4124 mL	2.0622 mL	4.1243 mL	10.3108 mL
	10 mM	0.2062 mL	1.0311 mL	2.0622 mL	5.1554 mL
	15 mM	0.1375 mL	0.6874 mL	1.3748 mL	3.4369 mL
	20 mM	0.1031 mL	0.5155 mL	1.0311 mL	2.5777 mL
	25 mM	0.0825 mL	0.4124 mL	0.8249 mL	2.0622 mL
	30 mM	0.0687 mL	0.3437 mL	0.6874 mL	1.7185 mL
	40 mM	0.0516 mL	0.2578 mL	0.5155 mL	1.2888 mL
	50 mM	0.0412 mL	0.2062 mL	0.4124 mL	1.0311 mL
	60 mM	0.0344 mL	0.1718 mL	0.3437 mL	0.8592 mL
	80 mM	0.0258 mL	0.1289 mL	0.2578 mL	0.6444 mL
	100 mM	0.0206 mL	0.1031 mL	0.2062 mL	0.5155 mL

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Sevabertinib

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EGFR アイソフォーム固有の製品をすべて表示

生物活性

化学情報

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Sevabertinib 関連分類

HY-164718 関連分類