Anticancer agent-361
Anticancer agent-361 is a glycine-conjugated coumarin-quinazoline fused heterocyclic derivative with selective antitumor proliferation activity. Anticancer agent-361 induces G0/G1 cell cycle arrest, apoptosis, and LDH release accompanied by membrane damage. Anticancer agent-361 is predicted to be a PI3Kα/PI3Kγ inhibitor. Anticancer agent-361 can be used for research on lung cancer, pancreatic cancer, prostate cancer, and breast cancer.
For research use only. We do not sell to patients.
- Formula: C23H18ClN5O6
- Molecular Weight:495.87
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Cellular Effect
|
Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| PANC-1 | IC50 |
3.77 μM
|
Cytotoxicity against human PANC-1 pancreatic carcinoma cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
Cytotoxicity against human PANC-1 pancreatic carcinoma cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
|
42617420 |
| A549 | IC50 |
3.57 μM
|
Cytotoxicity against human A549 lung carcinoma cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
Cytotoxicity against human A549 lung carcinoma cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
|
42617420 |
| PC-3 | IC50 |
5.21 μM
|
Cytotoxicity against human PC-3 prostate carcinoma cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
Cytotoxicity against human PC-3 prostate carcinoma cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
|
42617420 |
| MCF7 | IC50 |
6.07 μM
|
Cytotoxicity against human MCF-7 breast adenocarcinoma cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
Cytotoxicity against human MCF-7 breast adenocarcinoma cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
|
42617420 |
| HEK293 | IC50 |
11.10 μM
|
Cytotoxicity against non-tumorigenic human HEK-293 embryonic kidney cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
Cytotoxicity against non-tumorigenic human HEK-293 embryonic kidney cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
|
42617420 |
In Vitro
Anticancer agent-361 (Compound 9d) (0.5-200 μM; 48 h) exhibits IC50 = 3.57 μM against A549 cells, IC50 = 3.77 μM against PANC-1 cells, IC50 = 5.21 μM against PC-3 cells, and IC50 = 6.07 μM against MCF-7 cells, with selectivity indices (SI) of 3.11, 2.94, 2.13, and 1.83, respectively, relative to HEK-293 cells[1].
Anticancer agent-361 (IC50 concentration; 48 h) induces G0/G1 phase arrest in A549, PANC-1, PC-3, and MCF-7 tumor cells, with a decreased proportion of cells in S phase; it selectively induces late apoptosis in tumor cells; it causes moderate LDH release from tumor cells, while LDH leakage from HEK-293 cells remains low, suggesting that membrane damage is a secondary change following apoptosis[1].
Anticancer agent-361 exhibits favorable docking scores against PI3Kα, PI3Kγ, and RNR, with PI3Kα being the highest-scoring target, suggesting that PI3K inhibition is the more likely primary mechanism[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC-3, PANC-1, A549, MCF-7, HEK-293
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Concentration:IC50 values for the various cells
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Incubation Time:48 h
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Result:Triggered late‑stage apoptosis in tested tumor cells with weaker apoptotic response in HEK‑293 cells.
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Cell Line:PC-3, PANC-1, A549, MCF-7, HEK-293
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Concentration:IC50 values for the various cells
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Incubation Time:48 h
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Result:Induced G0/G1 phase accumulation and S‑phase reduction in A549, PANC‑1, PC‑3 and MCF‑7 tumor cells by flow‑cytometry cell‑cycle analysis.
Chemical Information
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Molecular Weight 495.87
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Formula C23H18ClN5O6
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SMILES
ClC1=CC=C(N=CN(CC(NNC(CNC(C2=CC(C=C(C)C=C3)=C3OC2=O)=O)=O)=O)C4=O)C4=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)