Diflomotecan
Diflomotecan (BN 80915) is a potent and orally active inhibitor of topoisomerase I. Diflomotecan (BN 80915) causes enhanced plasma stability and has the superior preclinical anti-tumour activity compared with other established compounds.
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- CAS. Nr.: 220997-97-7
- Formel: C21H16F2N2O4
- Molecular Weight:398.36
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
topoisomerase I[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
3.4 nM
Compound: 12
|
Cytotoxicity against human A549 cells by WST assay
Cytotoxicity against human A549 cells by WST assay
|
[PMID: 23578545] |
| A549 | IC50 |
3.4 nM
Compound: 8f
|
Cytotoxicity against A549 tumor cell line determined by WST-1 assay
Cytotoxicity against A549 tumor cell line determined by WST-1 assay
|
[PMID: 10841808] |
| HT-29 | IC50 |
8.4 nM
Compound: 8f
|
Cytotoxicity against HT-29 tumor cell line determined by WST-1 assay
Cytotoxicity against HT-29 tumor cell line determined by WST-1 assay
|
[PMID: 10841808] |
| T-24 | IC50 |
0.4 nM
Compound: 12
|
Cytotoxicity against human chemo-resistant T24 cells by WST assay
Cytotoxicity against human chemo-resistant T24 cells by WST assay
|
[PMID: 23578545] |
| T-24 | IC50 |
0.4 nM
Compound: 8f
|
Cytotoxicity against T24 tumor cell line determined by WST-1 assay
Cytotoxicity against T24 tumor cell line determined by WST-1 assay
|
[PMID: 10841808] |
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 220997-97-7
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Molecular Weight 398.36
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Formel C21H16F2N2O4
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SMILES
O=C(OC1)C[C@](O)(CC)C2=C1C(N3CC4=CC5=CC(F)=C(F)C=C5N=C4C3=C2)=O
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Synonyms
BN 80915
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Kroep JR, et al. Diflomotecan, a promising homocamptothecin for cancer therapy. Expert Opin Investig Drugs. 2009;18(1):69-75. [Content Brief]
[2]. Gelderblom H, et al. Phase I pharmacological and bioavailability study of oral diflomotecan (BN80915), a novel E-ring-modified camptothecin analogue in adults with solid tumors. Clin Cancer Res. 2003;9(11):4101-4107. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)