HUHS015 - CAS 1453097-13-6
Catalog number: 1453097-13-6
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
HUHS015 is a potent PCA-1/ALKBH3 inhibitor both in vitro and in vivo. The bioavailability (BA) of HUHS015 was 7.2% in rats after oral administration. As expected, continuously administering HUHS015 significantly suppressed the growth of DU145 cells, which are human hormone-independent prostate cancer cells, in a mouse xenograft model without untoward effects.
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white solid powder
HUHS015; HUHS 015; HUHS-015
1.Improving the bioavailability and anticancer effect of the PCA-1/ALKBH3 inhibitor HUHS015 using sodium salt.
Mabuchi M1, Shimizu T1, Ueda M1, Sasakawa Y2, Nakao S1, Ueda Y3, Kawamura A4, Tsujikawa K3, Tanaka A5. In Vivo. 2015 Jan-Feb;29(1):39-43.
Prostate cancer antigen (PCA)-1/AlkB homologue 3 (ALKBH3) has been identified as a clinically significant factor and siRNA of PCA-1 inhibits DU145 proliferation both in vitro and in vivo. HUHS015 ( 1: ), a previous reported PCA-1 small-molecule inhibitor, was also effective without any obvious side-effects or toxicity. The potency of HUHS015, however, is not satisfying. We thought the reason is poor solubility of HUHS015 because insoluble material remained at the injection site after subcutaneous administration. To improve this inhibitor's solubility, we prepared various salts of HUHS015 and examined their solubility, which resulted in the selection of HUHS015 sodium salt ( 2: ) for further studies in vivo. Next, we compared the pharmacokinetics of 1: and 2: via several administration routes. We observed significant improvements in the pharmacokinetic parameters. For example, subcutaneous administration of 2: increased the area under the curve (AUC)0-24 by 8-fold compared to 1 and increased the suppressive effect on the proliferation of DU145 cells in a xenograft model.
2.Design and synthesis of prostate cancer antigen-1 (PCA-1/ALKBH3) inhibitors as anti-prostate cancer drugs.
Nakao S1, Mabuchi M2, Shimizu T1, Itoh Y1, Takeuchi Y1, Ueda M1, Mizuno H2, Shigi N3, Ohshio I3, Jinguji K3, Ueda Y3, Yamamoto M4, Furukawa T4, Aoki S5, Tsujikawa K3, Tanaka A6. Bioorg Med Chem Lett. 2014 Feb 15;24(4):1071-4. doi: 10.1016/j.bmcl.2014.01.008. Epub 2014 Jan 11.
A series of 1-aryl-3,4-substituted-1H-pyrazol-5-ol derivatives was synthesized and evaluated as prostate cancer antigen-1 (PCA-1/ALKBH3) inhibitors to obtain a novel anti-prostate cancer drug. After modifying 1-(1H-benzimidazol-2-yl)-3,4-dimethyl-1H-pyrazol-5-ol (1), a hit compound found during random screening using a recombinant PCA-1/ALKBH3, 1-(1H-5-methylbenzimidazol-2-yl)-4-benzyl-3-methyl-1H-pyrazol-5-ol (35, HUHS015), was obtained as a potent PCA-1/ALKBH3 inhibitor both in vitro and in vivo. The bioavailability (BA) of 35 was 7.2% in rats after oral administration. As expected, continuously administering 35 significantly suppressed the growth of DU145 cells, which are human hormone-independent prostate cancer cells, in a mouse xenograft model without untoward effects.
3.Effect of loading rate on the apparent fracture toughness of acrylic bone cement.
Lewis G1. Biomed Mater Eng. 2002;12(2):149-55.
In this study, a determination is made of the effect of loading rate, v (0.1 mm min(-1) versus 1.0 mm min(-1) versus 10 mm min(-1)) on the value of the plane strain fracture toughness, K(Ic), of three commercial formulations of acrylic bone cement (Osteopal), CMW3, and Copal), that are characterized as "low-", "medium-", and "high-" viscosity brands, respectively). For all formulations, K(Ic) increases with increase in v. However, while this trend is statistically significant for CMW3 and Copal, this is not so for Osteopal. The CMW3 and Copal results are explained in terms of changes of the molecular relaxation transitions in the cement and the thermal state at the crack tip of the test specimen. Two implications of the findings are discussed. In the case of Osteopal, a recommendation for further study is made.
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CAS 1453097-13-6 HUHS015

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