P-gb-IN-1
P-gb-IN-1 (compound Ⅲ-8), a 2,5-disubstituted furan derivative, is a highly effective, broadspectrum P-glycoprotein (P-gp) inhibitor. P-gb-IN-1 displayed the reversal activity by inhibiting P-gp efflux. P-gb-IN-1 has a potent affinity to P-gp by forming H-bond interactions with residues Asn 721 and Met 986. P-gb-IN-1 possesses broad-spectrum reversal activity and low toxicity in MCF-7/ADR cells.
For research use only. We do not sell to patients.
- CAS No.: 2632874-49-6
- Formula: C30H28N2O6
- Molecular Weight:512.55
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| NCI/ADR-RES | IC50 |
0.09 μM
Compound: Cpd III-8
|
Cytotoxicity against human MCF7ADR cells assessed as doxorubicin IC50 at 5 uM incubated for 48 hrs by CCK8 assay
Cytotoxicity against human MCF7ADR cells assessed as doxorubicin IC50 at 5 uM incubated for 48 hrs by CCK8 assay
|
[PMID: 37229830] |
| NCI/ADR-RES | IC50 |
0.09 μM
Compound: Cpd III-8
|
Sensitization of doxorubicin-induced antitumor activity against human MCF7ADR cells assessed as doxorubicin IC50 at 5 uM incubated for 48 hrs by CCK8 assay
Sensitization of doxorubicin-induced antitumor activity against human MCF7ADR cells assessed as doxorubicin IC50 at 5 uM incubated for 48 hrs by CCK8 assay
|
[PMID: 37229830] |
| NCI/ADR-RES | IC50 |
0.36 μM
Compound: Cpd III-8
|
Sensitization of daunorubicin-induced antitumor activity against human MCF7ADR cells assessed as daunorubicin IC50 at 5 uM incubated for 48 hrs by CCK8 assay
Sensitization of daunorubicin-induced antitumor activity against human MCF7ADR cells assessed as daunorubicin IC50 at 5 uM incubated for 48 hrs by CCK8 assay
|
[PMID: 37229830] |
| NCI/ADR-RES | IC50 |
0.37 μM
Compound: Cpd III-8
|
Sensitization of paclitaxel-induced antitumor activity against human MCF7ADR cells assessed as paclitaxel IC50 at 5 uM incubated for 48 hrs by CCK8 assay
Sensitization of paclitaxel-induced antitumor activity against human MCF7ADR cells assessed as paclitaxel IC50 at 5 uM incubated for 48 hrs by CCK8 assay
|
[PMID: 37229830] |
| NCI/ADR-RES | IC50 |
0.53 μM
Compound: Cpd III-8
|
Sensitization of vincristine-induced antitumor activity against human MCF7ADR cells assessed as vincristine IC50 at 5 uM incubated for 48 hrs by CCK8 assay
Sensitization of vincristine-induced antitumor activity against human MCF7ADR cells assessed as vincristine IC50 at 5 uM incubated for 48 hrs by CCK8 assay
|
[PMID: 37229830] |
| NCI/ADR-RES | IC50 |
15.5 μM
Compound: Cpd III-8
|
Cytotoxicity against human MCF7ADR cells assessed as doxorubicin IC50 at 0.1 uM incubated for 48 hrs by CCK8 assay
Cytotoxicity against human MCF7ADR cells assessed as doxorubicin IC50 at 0.1 uM incubated for 48 hrs by CCK8 assay
|
[PMID: 37229830] |
| NCI/ADR-RES | IC50 |
5.78 μM
Compound: Cpd III-8
|
Cytotoxicity against human MCF7ADR cells assessed as doxorubicin IC50 at 0.5 uM incubated for 48 hrs by CCK8 assay
Cytotoxicity against human MCF7ADR cells assessed as doxorubicin IC50 at 0.5 uM incubated for 48 hrs by CCK8 assay
|
[PMID: 37229830] |
Chemical Information
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CAS No. 2632874-49-6
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Molecular Weight 512.55
-
Formula C30H28N2O6
-
SMILES
O=C(NC1=CC=C(C2=CC=C(C(N3CCC(C=C(OC)C(OC)=C4)=C4C3)=O)O2)C=C1)C5=CC=C(OC)C=C5
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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
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)