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製品番号: HY-187517

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Anticancer agent 357

Anticancer agent 357 is an orally active HER2 inhibitor. Anticancer agent 357 reduces the phosphorylation levels of HER2, AKT and GSK-3β, and downregulates the expression of β-catenin. Anticancer agent 357 inhibits the proliferation and migration of colon cancer cells with high HER2 expression, and suppresses tumor growth in xenograft models. Anticancer agent 357 can be used in colorectal cancer-related research.

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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。

分子式: C₂₀H₁₅F₃N₄
分子量:368.36

保管条件:

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

Anticancer agent 357 構造式

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
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
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
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生物活性

製品説明

IC₅₀ & Target

^[1]

HER2

GSK-3β

Akt

EGFR アイソフォーム固有の製品をすべて表示 :

Akt アイソフォーム固有の製品をすべて表示 :

GSK-3 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
NCM460	IC50	38.62 μM	Inhibition of cell viability against human normal colon epithelial NCM460 cells incubated for 24 hrs by CCK-8 assay. Inhibition of cell viability against human normal colon epithelial NCM460 cells incubated for 24 hrs by CCK-8 assay.	42492133
LS174T	IC50	24.17 μM	Inhibition of cell viability against human colon cancer LS174T cells incubated for 24 hrs by CCK-8 assay. Inhibition of cell viability against human colon cancer LS174T cells incubated for 24 hrs by CCK-8 assay.	42492133
HCT-116	IC50	29.74 μM	Inhibition of cell viability against human colon cancer HCT116 cells incubated for 24 hrs by CCK-8 assay. Inhibition of cell viability against human colon cancer HCT116 cells incubated for 24 hrs by CCK-8 assay.	42492133
NCM460	IC50	21.18 μM	Inhibition of cell viability against human normal colon epithelial NCM460 cells incubated for 72 hrs by CCK-8 assay. Inhibition of cell viability against human normal colon epithelial NCM460 cells incubated for 72 hrs by CCK-8 assay.	42492133
LS174T	IC50	9.57 μM	Inhibition of cell viability against human colon cancer LS174T cells incubated for 72 hrs by CCK-8 assay. Inhibition of cell viability against human colon cancer LS174T cells incubated for 72 hrs by CCK-8 assay.	42492133
HCT-116	IC50	9.71 μM	Inhibition of cell viability against human colon cancer HCT116 cells incubated for 72 hrs by CCK-8 assay. Inhibition of cell viability against human colon cancer HCT116 cells incubated for 72 hrs by CCK-8 assay.	42492133

体外実験

Anticancer agent 357 (compound 7) (0-40 μM; 24-72 h) inhibits the viability of LS174T and HCT116 colon cancer cells as well as NCM460 normal colonic epithelial cells in a dose- and time-dependent manner; after 72 h of incubation, its potency and selectivity against colon cancer cells are enhanced (IC₅₀ values: 9.57 μM for LS174T cells, 9.71 μM for HCT116 cells)^[1].
Anticancer agent 357 (20 μM; 24-48 h) significantly inhibits the proliferation and migration of LS174T and HCT116 colon cancer cells, as detected by scratch wound healing assay^[1].
Anticancer agent 357 (30 μM; 0-24 h) inhibits the HER2/AKT/GSK-3β/β-catenin signaling pathway in LS174T and HCT116 colon cancer cells by reducing the phosphorylation levels of HER2, AKT and GSK-3β, and downregulating β-catenin protein expression^[1].

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

Cell Viability Assay^[1]

Cell Line:

human colon cancer LS174T cells, human colon cancer HCT116 cells, human normal colon epithelial NCM460 cells
Concentration:

0, 1.5, 2.5, 5, 10, 20, 40 μM
Incubation Time:

24 h; 48 h; 72 h
Result:

Inhibited cell viability in all three cell lines in a concentration- and time-dependent manner.
Exhibited 24 h IC₅₀ values of 38.62 μM (NCM460), 24.17 μM (LS174T), and 29.74 μM (HCT116).
Exhibited 72 h IC₅₀ values of 21.18 μM (NCM460), 9.57 μM (LS174T), and 9.71 μM (HCT116).
Achieved selectivity index (SI) of 1.60 for LS174T and 1.30 for HCT116 at 24 h, and increased to 2.21 for LS174T and 2.18 for HCT116 at 72 h.

Cell Migration Assay ^[1]

Cell Line:

human colon cancer LS174T cells, human colon cancer HCT116 cells
Concentration:

20 μM
Incubation Time:

24 h
Result:

Markedly inhibited migratory capacity of LS174T and HCT116 cells.
Resulted in significantly lower percent wound closure in both cell lines relative to the vehicle control.

Cell Proliferation Assay^[1]

Cell Line:

human colon cancer LS174T cells, human colon cancer HCT116 cells
Concentration:

20 μM
Incubation Time:

48 h
Result:

Suppressed colony formation by LS174T and HCT116 cells.

Western Blot Analysis^[1]

Cell Line:

human colon cancer LS174T cells, human colon cancer HCT116 cells
Concentration:

30 μM
Incubation Time:

0, 2, 3, 4 h (HER2/AKT analysis)
0, 6, 9, 12 h (GSK-3β analysis)
24 h (β-catenin analysis)
Result:

Induced a time-dependent reduction in phosphorylation of HER2 (Tyr1221/1222) and AKT (Ser473) in both cell lines.
Caused a time-dependent decrease in phosphorylation of GSK-3β (Ser9) in both cell lines.
Downregulated β-catenin protein expression significantly in both cell lines after 24 h treatment relative to the control.

体内実験

Anticancer agent 357 (compound 7) (25-50 mg/kg; p.o.; daily; 14 days) significantly inhibits LS174T colorectal cancer xenograft growth in BALB/c nude mice, with the higher dose showing greater efficacy^[1].

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

Animal Model:

BALB/c nude mice (4-6 weeks old)^[1]
Dosage:

25 mg/kg; 50 mg/kg
Administration:

p.o.; daily; 14 days
Result:

Significantly inhibited LS174T xenograft tumor growth relative to vehicle control.
Did not cause significant body weight loss.
Exhibited a more pronounced inhibitory effect at 50 mg/kg than at 25 mg/kg.
Significantly reduced tumor weights in both treatment groups compared to vehicle control.\nSignificantly inhibited HCT116 xenograft tumor growth relative to vehicle control.
Did not cause significant body weight loss.
Significantly reduced tumor weights in both treatment groups compared to vehicle control.

化学情報

分子量 368.36
分子式 C₂₀H₁₅F₃N₄
SMILES

FC(F)(F)C1=CC=C(C2=NN3C(NCC[C@@H]3C4=CC=CC=C4)=C2C#N)C=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]. Wang D, et al. Anticancer evaluation of novel chiral tetrahydropyrazolo[1,5-a]pyrimidine derivatives: Inhibitory effects on proliferation and migration of colon cancer cells with high HER2 expression. Bioorg Chem. 2026 Jul 15;181:110251.

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.

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MOQ

Minimum order quantity

100 mg

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