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Biological Activity:

Vismodegib (GDC-0449) is a potent and specific hedgehog pathway inhibitor with an IC₅₀ of 3 nM. It has been approved by FDA to treat BCC, and also in multiple clinical trials to treat advanced solid tumors. It blocks the activities of the Hedgehog-ligand cell surface receptors PTCH and/or SMO and suppressing Hedgehog signaling. It prevents multiple ATP-binding cassette (ABC) transporters. GDC-0449 also exhibited efficacy in medulloblastoma animal models and primary pancreatic cancer xenograft models. It was shown to inhibit cell growth in cisplatin-resistant lung cancer cells.

How to Use:

• In vitro: GDC-0449 was used at 5-10 μM concentration in the cellular assays.
• In vivo: GDC-0449 was dosed orally 12.5 mg/kg twice per day (lowest dose), up to 100 mg/kg twice per day (formulated as a suspension in 0.5% methylcellulose, 0.2% Tween-80 (MCT))?

Reference:

1. 1. Robarge KD, et al. GDC-0449-a potent inhibitor of the hedgehog pathway. (2009) Bioorg Med Chem Lett. 19(19):5576-81.
2. 2. Yauch RL, et al. Smoothened mutation confers resistance to a Hedgehog pathway inhibitor in medulloblastoma. (2009) Science 326(5952):572-4.
3. 3. LoRusso PM, et al. Phase I trial of hedgehog pathway inhibitor vismodegib (GDC-0449) in patients with refractory, locally advanced or metastatic solid tumors. ?(2011) Clin Cancer Res.17(8):2502-11
4. 4. Giannetti AM, et al. Identification, characterization, and implications of species-dependent plasma protein binding for the oral Hedgehog pathway inhibitor vismodegib (GDC-0449). (2011) J Med Chem. 54(8):2592-601
5. 5. Lorusso PM, et al. Pharmacokinetic dose-scheduling study of hedgehog pathway inhibitor vismodegib (GDC-0449) in patients with locally advanced or metastatic solid tumors. (2011) Clin Cancer Res. 17(17):5774-82
6. 6. Philips GM, et al. Hedgehog signaling antagonist promotes regression of both liver fibrosis and hepatocellular carcinoma in a murine model of primary liver cancer.(2011) PLoS One. 6(9):e23943.
7. 7. Metcalfe C, et al. Hedgehog fights back: mechanisms of acquired resistance against Smoothened antagonists. ?(2011) Cancer Res. 71(15):5057-61.
8. 8. Singh BN, et al. Hedgehog signaling antagonist GDC-0449 (Vismodegib) inhibits pancreatic cancer stem cell characteristics: molecular mechanisms. (2011) PLoS One. 6(11):e27306
9. 9. Tian F, et al. The hedgehog pathway inhibitor GDC-0449 alters intracellular Ca2+ homeostasis and inhibits cell growth in cisplatin-resistant lung cancer cells. ?(2012) Anticancer Res. 32(1):89-94

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