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Valrubicin

Valrubicin is a semisynthetic anthracycline antitumor antibiotic and derivative of doxorubicin.<sup class="referenceList">[1]</sup> It inhibits the growth of human bladder tumor cell lines with LD50 values ranging from 0.05 to 11.2 μM.<sup class="referenceList">[2]</sup> Valrubicin is more active against cells in the plateau growth phase than in the log growth phase (LD70s = 2.5 and 12.1 μM, respectively for CUB-2 cells). Valrubicin (40 mg/kg) increases survival in mice with murine P388 and L1210 leukemias.<sup class="referenceList">[1]</sup> Topical administration of valrubicin (0.01 g/ml) reduces epidermal thickness and normalizes epidermal morphology in a mouse psoriasis xenograft transplantation model.<sup class="referenceList">[3]</sup> Formulations containing valrubicin have been used in the treatment of bladder cancer.
56124-62-0
Item No.
TX00DFH5
CAS No.
56124-62-0
Molecular Formula
C34H36F3NO13
Molecular Weight
723.6437
Pricing ＆ Availability
Pack Size Purity Price(USD) Availability Quantity
1mg 95% $30.00 in stock
5mg 98% $58.00 in stock
10mg 98% $78.00 in stock
25mg 98% $102.00 in stock
50mg 98% $171.00 in stock
100mg 98% $289.00 in stock
250mg 98% $519.00 in stock
WARNING This product is for research use only. SDS
Technical Information
Item No.:
TX00DFH5
Product Name:
Valrubicin
Description:
Synonyms:
NSC 246131; N-Trifluoroacetyladriamycin-14-valerate; Valrubicin
CAS Number:
56124-62-0
MDL:
MFCD01939322
Molecular Formula:
C34H36F3NO13
Molecular Weight:
723.6437
SMILES:
OC1=C(C[C@](C(COC(CCCC)=O)=O)(O)C[C@@H]2O[C@@](O[C@@H](C)[C@H]3O)([H])C[C@@H]3NC(C(F)(F)F)=O)C2=C(O)C(C4=O)=C1C(C5=CC=CC(OC)=C45)=O
λmax:
201, 235, 252, 496 nm
IC₅₀ & Target:
TPA-activated PKC PDBu-activated PKC
0.85 μM (IC50) 1.25 μM (IC50)
Cell Assay:
UMSCC5 cells exposed to Valrubicin (2 μM for 3 h), a single dose of radiation (400 cGy), or the combined treatment are cultured for a further 12, 24, or 48 hours. At these times, the cells are collected by trypsinization (0.25%), washed in phosphate-buffered saline (PBS), and fixed at 5 × 106 cells/mL with 95% ethanol. Cells are incubated with ribonuclease (50 μg; 70-90 Kunitz units/mg for 30 min), and the resulting pellet resuspended in and incubated with propidium iodide (0.05 mg/mL for 10 min). The DNA content of the samples is determined by flow cytometry according to standard technique[2]. Method(s) not verified, for reference only.
Animal Administration:
Hamsters[2] Hamsters with cheek pouch tumors of 100 mm2 are randomly assigned to one of five treatment groups. Momentarily anesthetized animals each receives once a week × 3 injections (27 g × 0.5-inch needle: 0.1 mL administered slowly to the base of the lesion) of Valrubicin (3, 6, or 9 mg) or drug vehicle (Cremophor: alcohol;1:1 by volume; NCl diluent 12). A further group of animals receives anesthesia but no direct tumor treatment (control). Individual tumor sizes are measured with calipers at weekly intervals for 4 weeks, at which time the animals are sacrificed[2]. Method(s) not verified, for reference only.
Solubility:
: , DMF: 5 mg/ml, DMSO: 5 mg/ml, Ethanol: 5 mg/ml
Shipping Condition:
Room temperature in continental US; may vary elsewhere.
References & Citations:
[1]. 1.Israel, M., Modest, E.G., and Frei, E., III N-trifluoroacetyladriamycin-14-valerate, an analog with greater experimental antitumor activity and less toxicity than adriamycin Cancer Res. 35(5),1365-1368 (1975).
[2]. Rosada, C., Stenderup, K., de Darkó, E., et al. Valrubicin in a topical formulation treats psoriasis in a xenograft transplantation model J. Invest. Dermatol. 130(2),455-463 (2010).
[3]. Niell, H.B., Hunter, R.F., Herrod, H.G., et al. Effects of N-trifluoroacetyladriamycin-14-valerate (AD-32) on human bladder tumor cell lines Cancer Chemother. Pharmacol. 19(1),47-52 (1987).