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製品番号: HY-111250

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SYR127063

SYR127063 is a potent and selective human epidermal growth factor receptor 2 (HER2) tyrosine kinase inhibitor with an IC₅₀ of 11 nM. SYR127063 binds to the active site of the HER2 kinase domain in an ATP-competitive manner, thereby preventing the formation of the conserved salt bridge required for kinase activation. SYR127063 can be used in research related to breast cancer, ovarian cancer and gastric cancer.

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CAS 番号: 871026-18-5
分子式: C₂₃H₂₀ClF₃N₄O₃
分子量:492.88

保管条件:

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

SYR127063 構造式

CAS 番号: 871026-18-5

価格（税別）

Amount: USD 0.00

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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
- IC₅₀ & Target
- Cellular Effect
- 体外実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

^[1]

HER2

11 nM (IC₅₀)

HER4

>10000 nM (IC₅₀)

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
BT-474	GI₅₀	27 nM Compound: 12j	Growth inhibition of human BT474 cells overexpressing HER2 gene after 5 days by particle analyzer Growth inhibition of human BT474 cells overexpressing HER2 gene after 5 days by particle analyzer	[PMID: 22003817]

体外実験

SYR127063 (preincubated for 5 min followed by a 10 min reaction with ATP) potently and selectively inhibits purified human HER2 kinase, with an IC₅₀ of 11 nM. Its activity against human EGFR is approximately 40-fold weaker, and it shows no significant activity against human HER4^[1].
SYR127063 (1 mM; incubated on ice for 1 h before use for crystallization, used to observe the resting state) binds to the ATP pocket and stabilizes a specific conformation of HER2 in a cell-free system^[1].
SYR127063 binds tightly to the intracellular kinase domain (HER2in) of human HER2, with an average binding affinity of -11.0 kcal/mol, and forms stable interactions with the binding site in subdomain II of this receptor^[2].

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

Related Protocols :

Breast Cancer Modeling

化学情報

CAS 番号 871026-18-5
分子量 492.88
分子式 C₂₃H₂₀ClF₃N₄O₃
SMILES

FC(F)(F)C=1C=CC=C(OC2=CC=C(C=C2Cl)NC3=NC=NC=4C=CN(C43)CCOCCO)C1
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

取扱説明書 (2659 KB)

参考文献

[1]. Aertgeerts K, et al. Structural analysis of the mechanism of inhibition and allosteric activation of the kinase domain of HER2 protein. The Journal of biological chemistry. 2011 May 27;286(21):18756-65. [Content Brief]

[2]. Hakaman, H., et al. In-Silico molecular docking analysis of monoclonal antibodies, approved inhibitors, and plant-based inhibitors targeting extracellular and intracellular HER2 receptor. Berkala Penelitian Hayati, 31(1), 33–48.

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

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)

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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