Vismodegib (GDC-0449)

Catalog No.S1082

Vismodegib (GDC-0449) is a potent, novel and specific hedgehog inhibitor with IC50 of 3 nM and also inhibits P-gp with IC50 of 3.0 μM in a cell-free assay.

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Vismodegib (GDC-0449) Chemical Structure

Vismodegib (GDC-0449) Chemical Structure
Molecular Weight: 421.3

Validation & Quality Control

Cited by 34 publications:

15 customer reviews :

Quality Control & MSDS

Related Compound Libraries

Vismodegib (GDC-0449) is available in the following compound libraries:

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Product Information

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  • Research Area

Product Description

Biological Activity

Description Vismodegib (GDC-0449) is a potent, novel and specific hedgehog inhibitor with IC50 of 3 nM and also inhibits P-gp with IC50 of 3.0 μM in a cell-free assay.
Targets Hedgehog [1]
(Cell-free assay)
IC50 3 nM
In vitro GDC-0449 targets the Hedgehog signaling pathway, blocking the activities of the Hedgehog-ligand cell surface receptors PTCH and/or SMO and suppressing Hedgehog signaling. GDC-0449 prevents multiple ATP-binding cassette (ABC) transporters. GDC-0449 also blocks ABCG2, Pgp, and MRP1-important ABC transporters associated with MDR. GDC-0449 is a potent inhibitor of ABC transporters, ABCG2/BCRP and ABCB1/Pgp, and is a mild inhibitor of ABCC1/MRP1. In ABCG2-overexpressing HEK293 cells, GDC-0449 increases retention of the fluorescent ABCG2 substrate BODIPY-prazosin and resensitizes these cells to mitoxantrone. In Madin-Darby canine kidney II cells engineered to overexpress Pgp or MRP1, GDC-0449 increases the retention of calcein-AM and resensitizes them to colchicine. GDC-0449 also resensitizes human non-small cell lung carcinoma cells NCI-H460/par and NCI-H460/MX20, which overexpress ABCG2 in response to mitoxantrone, to mitoxantrone, and to topotecan or SN-38. The IC50 values of GDC-0449 for prevention of ABCG2 and Pgp are about 1.4 μM and 3.0 μM, respectively. [2] GDC-0449 alters intracellular Ca2+ homeostasis and inhibits cell growth in cisplatin-resistant lung cancer cells. [3]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
Sk-ChA-1 M4X6RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M4TsVFAvOjYkgKO1NEDPxE1?MWi3NkBpMUXJR|UxRTd2LkW0xtEzNjV6zszNMVOyOVc1OjR6Mh?=
Smo-D473H M4C1XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MnXmTWM2OMLib3[gO{4yyqEQvF2=M1H1VVI1OjlzMUC0
T315I BCR-ABL BaF3NGrMfHZHfW6ldHnvckBCe3OjeR?=MWexNEDPxE1?MW[3NkBpNGHjOFZz\WS3Y3XzJJRp\SCneIDy[ZN{cW:wIH;mJGdtcTIEoB?=NUn3[|kzOjN|MUm4NlQ>

... Click to View More Cell Line Experimental Data

In vivo GDC-0449 has been used to treat medulloblastoma in animal models. [2] GDC-0449 prevents the growth of primary pancreatic xenografts without non-specifically inhibiting pancreatic cell proliferation. Oral dosing of GDC-0449 causes tumor regressions in the Ptch(+/-) allograft model of medulloblastoma at doses ≥25 mg/kg and tumor growth inhibition at doses up to 92 mg/kg dosed twice daily in two ligand-dependent colorectal cancer models, D5123, and 1040830. Analysis of Hh pathway activity and PK/PD modeling reveals that GDC-0449 inhibits Gli1 with a similar IC50 in both the medulloblastoma and D5123 models (0.165 μM and 0.267 μM, respectively). Pathway modulation is linked to efficacy using an integrated PK/PD model revealing a steep relationship where > 50% of the activity of GDC-0449 is associated with >80% repression of the Hh pathway. [4]

Protocol(Only for Reference)

Cell Assay: [2]

Cell lines MDCKII cells
Concentrations 20 μM
Incubation Time 2 hours
Method MDCKII cells are seeded into 24-well plates at a density of 3 × 105 cells per well and are allowed to attach. Medium is then changed to that containing different drugs (50 μM VP, 50 μM indomethacin, or 20 μM GDC-0449 in DMSO or DMSO alone as control, and nonfluorescent calcein-AM is added to a final concentration of 1.0 μM and incubated at 37 °C for 2 hours. Cells are then washed twice with Ca2+, Mg2+-containing Hank's balanced salt solution buffer and lysed by shaking in 0.01% Triton X-100 in PBS buffer for 1 hour at room temperature or overnight at 4 °C. The lysate is then transferred into 96-well plates, and the fluorescence signal caused by the cell-derived calcein is quantified spectrophotometrically with a SpectraMax M5 Multi-Detection Readerusing an excitation wavelength of 495 nm and an emission wavelength of 515 nm. All manipulations are performed in the dark. All readings are expressed as mean ?SEM normalized to the control.

Animal Study: [4]

Animal Models Ptch(+/-) allograft model, D5123 and 1040830
Formulation In 0.5% methyl-cellulose, 0.2% tween-80
Dosages ~ 100 mg/kg
Administration Orally

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Scales SJ, et al. Trends Pharmacol Sci. 2009, 30(6), 303-312.

[2] Zhang Y, et al. Neoplasia. 2009, 11(1), 96-101.

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Clinical Trial Information( data from, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
Start Date Phases
NCT02366312 Active, not recruiting Keratocystic Odontogenic Tumor The Bluestone Center for Clinical Research|Genentech, Inc. June 2016 Phase 2
NCT02694224 Recruiting Breast Cancer Clinica Universidad de Navarra, Universidad de Navarra April 2016 Phase 2
NCT02693535 Recruiting Lymphoma, Non-Hodgkin|Multiple Myeloma|Advanced Solid Tumors American Society of Clinical Oncology|AstraZeneca|Bayer|B  ...more American Society of Clinical Oncology|AstraZeneca|Bayer|Bristol-Myers Squibb|Eli Lilly and Company|Genentech, Inc.|Merck Sharp & Dohme Corp.|Pfizer March 2016 Phase 2
NCT02690948 Recruiting Skin Basal Cell Carcinoma Anne Chang|Merck Sharp & Dohme Corp.|National Cancer Inst  ...more Anne Chang|Merck Sharp & Dohme Corp.|National Cancer Institute (NCI)|Stanford University February 2016 Phase 2
NCT02648048 Recruiting Idiopathic Pulmonary Fibrosis Hoffmann-La Roche January 2016 Phase 1

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Chemical Information

Download Vismodegib (GDC-0449) SDF
Molecular Weight (MW) 421.3


CAS No. 879085-55-9
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 84 mg/mL (199.38 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 2% DMSO+30% PEG 300+5% Tween 80+ddH2O 10mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 2-chloro-N-(4-chloro-3-(pyridin-2-yl)phenyl)-4-(methylsulfonyl)benzamide

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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