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5HPP-33

Cat. No. M7843
5HPP-33 Structure
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Biological Activity

5HPP-33 is a thalidomide derivative which was reported to be active as anticancer agent through stabilization of the microtubules. 5HPP-33 has shown inhibition of cell proliferation of both estrogen-dependent (MCF-7) and estrogen-independent (MDA-MB-231) breast cancer cells as well as other cell lines. A study in tubulin forming assay reported that 5HPP-33 acts as a microtubule formation inhibitor (IC50=810 nM).

Chemical Information
Molecular Weight 323.39
Formula C20H21NO3
CAS Number 105624-86-0
Solubility (25°C) DMSO: ≥20 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Aijaz Rashid, et al. Thalidomide (5HPP-33) suppresses microtubule dynamics and depolymerizes the microtubule network by binding at the vinblastine binding site on tubulin

[2] Bulbul Pandit, et al. Structure-activity relationship studies of thalidomide analogs with a taxol-like mode of action

[3] Nicole Kleinstreuer, et al. A computational model predicting disruption of blood vessel development

[4] Masahiro Kizaki, et al. New tubulin polymerization inhibitor derived from thalidomide: implications for anti-myeloma therapy

[5] Toyotaka Iguchi, et al. Novel tubulin-polymerization inhibitor derived from thalidomide directly induces apoptosis in human multiple myeloma cells: possible anti-myeloma mechanism of thalidomide

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Keywords: 5HPP-33 supplier, inhibitors, activators


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