Detorubicin
Detorubicin (NSC 292652; RP 33921) is a semi-synthetic anthracycline anticancer agent and a hydrophobic prodrug of Doxorubicin (HY-15142A). Detorubicin enters cancer cells faster and achieves higher intracellular levels than Doxorubicin. Detorubicin localizes exclusively to lysosomes and the nucleus, with unmetabolized Detorubicin accumulating mainly in lysosomes. Detorubicin can be used in research related to hematologic malignancies and L1210 leukemia.
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- CAS No.: 66211-92-5
- 화학식: C33H39NO14
- 분자량:673.67
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
Detorubicin (20-120 min) exhibits pH-dependent stability, with the highest stability at pH 4.5, intermediate stability at pH 6.5, and the lowest stability at pH 7.4[2].
Detorubicin (10-85 μM; 20-120 min) is taken up faster and reaches higher intracellular levels than doxorubicin in L1210 leukemia cells, with intact detorubicin plateauing at 30 min and total anthracycline fluorescence plateauing at 120 min when incubated with 85 μM detorubicin[2].
Detorubicin (85 μM; 20-120 min) localizes primarily to lysosomes in L1210 leukemia cells, while its hydrolysis product doxorubicin localizes primarily to the nucleus, with nuclear doxorubicin levels reaching 5.44 μg/mg cell protein after 120 min[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:L1210 leukemia cells
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Concentration:85 μM
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Incubation Time:20 min, 120 min
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Result:Was present at 0.75 μg/mg cell protein in post-nuclear supernatant and 0.81 μg/mg cell protein in nuclear fraction after 20 min incubation.
Was present at 1.40 μg/mg cell protein in post-nuclear supernatant and 1.23 μg/mg cell protein in nuclear fraction after 120 min incubation.
Localized 61% to lysosomes and 39% to DNA in post-nuclear supernatant after 20 min incubation, shifting to 98% in lysosomes and 2% in DNA after 120 min incubation.
Had hydrolysis product doxorubicin present at 0.69 μg/mg cell protein in post-nuclear supernatant and 2.12 μg/mg cell protein in nuclear fraction after 20 min incubation.
Had hydrolysis product doxorubicin present at 1.21 μg/mg cell protein in post-nuclear supernatant and 5.44 μg/mg cell protein in nuclear fraction after 120 min incubation.
Had hydrolysis product doxorubicin localize 22% to lysosomes and 78% to DNA in post-nuclear supernatant after 20 min incubation, shifting to 39% in lysosomes and 61% in DNA after 120 min incubation.
Chemical Information
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CAS No. 66211-92-5
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분자량 673.67
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화학식 C33H39NO14
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SMILES
OC=1C2=C([C@@H](O[C@H]3C[C@H](N)[C@H](O)[C@H](C)O3)C[C@@](C(COC(C(OCC)OCC)=O)=O)(O)C2)C(O)=C4C1C(=O)C=5C(C4=O)=C(OC)C=CC5
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Synonyms
NSC 292652; RP 33921
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[1]. Deprez-de Campeneere D, et al.. Accumulation and metabolism of new anthracycline derivatives in the heart after IV injection into mice. Cancer chemotherapy and pharmacology. 1982;8(2):193-7. [Content Brief]
[2]. Zenebergh A, et al.. Cellular pharmacology of detorubicin and doxorubicin in L1210 cells. European journal of cancer & clinical oncology. 1984 Jan;20(1):115-21. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Detorubicin Related Classifications
HY-106414 Related Classifications
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