GDC-0449 (Vismodegib)

GDC-0449 (Vismodegib)

Catalog Number:
L002368480APE
Mfr. No.:
APE-A3021
Price:
$188
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      • Overview
        • Please contact us at for specific academic pricing.

          Background

          GDC-0449 (2-chloro-N-[4-chloro-3-pyridin-2-yl-phenyl]-4-methane-sulfonyl benzamide), discovered by high throughput screening of a small molecule compound library followed by subsequent optimization through medical chemistry, is a potent and selective inhibitor of hedgehog (Hh) signaling, a pathway regulating cell growth and differentiation associated in pathogenesis of several cancers. It binds to signaling by smoothened (SMO) and suppresses activation of downstream Hh target genes resulting in the inhibition of Hh signaling pathway. GDC-0449 exhibits anti-tumor activity in a mouse model of medulloblastoma as well as in primary human tumor cell xenograft models of colorectal cancer and pancreatic carcinoma and is currently being evaluated in research projects investigating refractory, locally advanced or metastatic solid tumors.

      • Properties
        • Categories
          Hedgehog antagonist, potent and selective
          Alternative Name
          Vismodegib, GDC-0449, HhAntag691, GDC0449, GDC 0449; 2-chloro-N-(4-chloro-3-pyridin-2-ylphenyl)-4-methylsulfonylbenzamide
          CAS Number
          879085-55-9
          Molecular Formula
          C19H14Cl2N2O3S
          Molecular Weight
          421.3
          Appearance
          A solid
          Purity
          98.00%
          Solubility
          ≥21.08 mg/mL in DMSO; insoluble in H2O; ≥4.96 mg/mL in EtOH with gentle warming and ultrasonic
          Storage
          Desiccate at -20°C
          SMILES
          CS(=O)(=O)C1=CC(=C(C=C1)C(=O)NC2=CC(=C(C=C2)Cl)C3=CC=CC=N3)Cl

          * For Research Use Only

      • Reference
        • 1. Su-Fen Wei, Dan-Hua He, et al. "Identification of pseudolaric acid B as a novel Hedgehog pathway inhibitor in medulloblastoma." Biochem Pharmacol. 2021 Aug;190:114593. PMID:33964282
          2. Kowolik CM, Lin M, et al. "Attenuation of hedgehog/GLI signaling by NT1721 extends survival in pancreatic cancer." J Exp Clin Cancer Res. 2019 Oct 28;38(1):431. PMID:31661013
          3. Lima-Fernandes E, Murison A, et al. "Targeting bivalency de-represses Indian Hedgehog and inhibits self-renewal of colorectal cancer-initiating cells." Nat Commun. 2019 Mar 29;10(1):1436. PMID:30926792

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