Vismodegib, Free Base **

产品名称：Vismodegib, Free Base
产品货号：LC  V-4050
产品规格：1 G
Vismodegib (GDC-0449) is a potent hedgehog (Hh) signaling pathway inhibitor.
The overexpression of ATP-binding cassette (ABC) transporters is associated with multidrug resistance.  Vismodegib is a potent inhibitor of two ABC transporters, ABCG2/BCRP and ABCB1/Pgp, with IC50 values of 1.4 and 3.0 µM, respectively.  Zhang, Y., et al.  "Hedgehog pathway inhibitor HhAntag691 is a potent inhibitor of ABCG2/BCRP and ABCB1/Pgp."  Neoplasia 11:  96-101 (2009).
A phase 1 clinical trial demonstrated that vismodegib had antitumor activity in locally advanced or metastatic basal-cell carcinoma.  Von Hoff, D.D., et al.  "Inhibition of the hedgehog pathway in advanced basal-cell carcinoma."  N. Engl. J. Med. 361:  1164-1172 (2009).
The treatment with vismodegib of a 26-year-old man with metastatic medulloblastoma that was refractory to multiple therapies resulted in rapid but transient regression of the tumor and relief of symptoms.  Rudin, C.M., et al.  "Treatment of medulloblastoma with hedgehog pathway inhibitor GDC-0449."  N. Engl. J. Med. 361:  1173-1178 (2009).
Vismodegib at doses as low as 12.5 mg/kg BID caused complete tumor regression in a medulloblastoma allograft mouse model which is dependent on the Hh pathway for growth.  Robarge, K.D., et al.  "GDC-0449-a potent inhibitor of the hedgehog pathway."  Bioorg. Med. Chem. Lett. 19:  5576-5581 (2009).
Acquired mutations in Smoothened (SMO), a serpentine receptor, inhibited the ability of vismodegib to bind SMO and served as a mechanism of drug resistance in human cancer.  Yauch, R.L., et al.  "Smoothened mutation confers resistance to a Hedgehog pathway inhibitor in medulloblastoma."  Science 326:  5576-5581 (2009).
Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO at 200 mg/mL; soluble in ethanol at 10 mg/mL with warming; very poorly soluble in water; maximum solubility in plain water is estimated to be about 10-20 µM buffers, serum, or other additives may increase or decrease the aqueous solubility.  Disposal:  A

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