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Cat. No.: 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.

For research use only. We do not sell to patients.

Formula: C₂₀H₁₅F₃N₄
Molecular Weight:368.36

Storage:

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

Anticancer agent 357 Chemical Structure

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Antibody-Drug Conjugates

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Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

IC₅₀ & Target^[1]

HER2

GSK-3β

Akt

All EGFR Isoforms :

All Akt Isoforms :

All GSK-3 Isoforms :

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

In Vitro

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.

In Vivo

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.

Chemical Information

Molecular Weight 368.36
Formula C₂₀H₁₅F₃N₄
SMILES

FC(F)(F)C1=CC=C(C2=NN3C(NCC[C@@H]3C4=CC=CC=C4)=C2C#N)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[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.

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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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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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Anticancer agent 357

All EGFR Isoforms

All Akt Isoforms

All GSK-3 Isoforms