xl-888 and Neoplasms

xl-888 has been researched along with Neoplasms* in 1 studies

Other Studies

1 other study(ies) available for xl-888 and Neoplasms

Article	Year
Discovery of XL888: a novel tropane-derived small molecule inhibitor of HSP90. Bioorganic & medicinal chemistry letters, 2012, Sep-01, Volume: 22, Issue:17 With structural guidance, tropane-derived HTS hits were modified to optimize for HSP90 inhibition and a desirable in vivo profile. Through an iterative SAR development process 12i (XL888) was discovered and shown to reduce HSP90 client protein content in PD studies. Furthermore, efficacy experiments performed in a NCI-N87 mouse xenograft model demonstrated tumor regression in some dosing regimens. Topics: Animals; Antineoplastic Agents; Azabicyclo Compounds; Cell Line, Tumor; Cell Proliferation; Crystallography, X-Ray; Drug Discovery; HSP90 Heat-Shock Proteins; Humans; Mice; Models, Molecular; Neoplasms; Phthalic Acids	2012

Article

Year

Discovery of XL888: a novel tropane-derived small molecule inhibitor of HSP90.

Bioorganic & medicinal chemistry letters, 2012, Sep-01, Volume: 22, Issue:17

With structural guidance, tropane-derived HTS hits were modified to optimize for HSP90 inhibition and a desirable in vivo profile. Through an iterative SAR development process 12i (XL888) was discovered and shown to reduce HSP90 client protein content in PD studies. Furthermore, efficacy experiments performed in a NCI-N87 mouse xenograft model demonstrated tumor regression in some dosing regimens.

Topics: Animals; Antineoplastic Agents; Azabicyclo Compounds; Cell Line, Tumor; Cell Proliferation; Crystallography, X-Ray; Drug Discovery; HSP90 Heat-Shock Proteins; Humans; Mice; Models, Molecular; Neoplasms; Phthalic Acids

2012