Vismodegib (GDC-0449)

Catalog No.S1082

Vismodegib (GDC-0449) Chemical Structure

Molecular Weight(MW): 421.3

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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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.
Hedgehog [1]
(Cell-free assay)
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 Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCE-T NHfvWGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnS4TWM2OD1zLkOyNlQ4KM7:TR?= M{TCbHNCVkeHUh?=
D-542MG M3\GRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13mSmlEPTB;MT64Olc{PyEQvF2= M4fmUXNCVkeHUh?=
23132-87 NFOzSllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2n0dWlEPTB;ND60NFE1PyEQvF2= MorLV2FPT0WU
ACN M{W0dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRThwNUCxNFkh|ryP M4e5XHNCVkeHUh?=
HuO-3N1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXRTWM2OD17Lk[wNVA5KM7:TR?= M2PVTHNCVkeHUh?=
BHT-101 NHfQNm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfCVJpKSzVyPUGxMlM5KM7:TR?= MlXEV2FPT0WU
D-423MG MlSwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;ndGlEPTB;MUKuO|Y2PyEQvF2= M2WwcnNCVkeHUh?=
HOS M121PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;ZTWM2OD1zNT62O|E6KM7:TR?= MXTTRW5ITVJ?
NB7 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1roSGlEPTB;MUWuPFkyKM7:TR?= NEP4fY9USU6JRWK=
DMS-273 M1j4RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{Ll[GlEPTB;MU[uOlcyOyEQvF2= MkG1V2FPT0WU
MDA-MB-361 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1z3b2lEPTB;MUeuNlcyOSEQvF2= NYfHZWtDW0GQR1XS
DU-145 NHHjOnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETtS2dKSzVyPUG4MlMzKM7:TR?= MV;TRW5ITVJ?
NCI-H82 NELmc41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjhPHhKSzVyPUG5Mlg{QDZizszN MUjTRW5ITVJ?
NCI-SNU-1 M4jkUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLtflRKSzVyPUKwMlAyQTZizszN NELVRlJUSU6JRWK=
C2BBe1 Mn[5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTJzLkGwOVgh|ryP MXrTRW5ITVJ?
LB2241-RCC MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrTVFQ2UUN3ME2yNU45PDRzIN88US=> M4rWVnNCVkeHUh?=
COLO-829 NX\TTpFpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTJ{LkG4O|Eh|ryP NXe3XphNW0GQR1XS
EW-11 M4TSWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWSyNlJqUUN3ME2yNk45ODJ{IN88US=> NYj0O|d5W0GQR1XS
NCI-H526 NGTrVW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjiXXpKSzVyPUKzMlQ4OTdizszN MnzPV2FPT0WU
SF295 MkO2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTJ2LkCyOVIh|ryP MWHTRW5ITVJ?
8505C NEL5co1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLBPI17UUN3ME2yOU43OzNzIN88US=> MYXTRW5ITVJ?
HT-29 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXR[2xKSzVyPUK2MlA1OzFizszN NXXpUmhrW0GQR1XS
NBsusSR MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDJTWM2OD1{Nj64NFA3KM7:TR?= MnLOV2FPT0WU
BV-173 MnLaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nsXGlEPTB;MkiuN|E5OiEQvF2= NET3NpdUSU6JRWK=
CTB-1 M3znOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDE[2pKSzVyPUOwMlExOzFizszN NGjGT2RUSU6JRWK=
JAR M{nM[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkW1TWM2OD1|Mj61N|cyKM7:TR?= MV3TRW5ITVJ?
CAL-51 NVPSd4M5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{GxXWlEPTB;M{SuO|E4PiEQvF2= NYrsSmpmW0GQR1XS
A172 M2DTU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4eybGlEPTB;M{euOFkzOSEQvF2= MlX2V2FPT0WU
MKN7 M4LxRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2DQV2lEPTB;M{muNFA4QSEQvF2= M13pdnNCVkeHUh?=
ONS-76 M2LrbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TFPGlEPTB;NEOuN|A2PyEQvF2= MVjTRW5ITVJ?
RS4-11 M3iyc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrMWWxSUUN3ME20OE4xPzV{IN88US=> NVPs[IZ7W0GQR1XS
NOS-1 M1LlOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTDTWM2OD12ND62NFMyKM7:TR?= MlrFV2FPT0WU
A101D NF7KTG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoH1TWM2OD12ND64NFI{KM7:TR?= MXPTRW5ITVJ?
HCC1806 NFr3cZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEi5cIxKSzVyPUS2MlEyPDhizszN M3jCenNCVkeHUh?=
CAL-27 Mmr4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTR5LkeyOFYh|ryP M1LVZnNCVkeHUh?=
OVCAR-4 NE\GdYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnXclI5UUN3ME21NE4xPjBzIN88US=> NVPxU2pSW0GQR1XS
HD-MY-Z M1fXbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTVyLke3OlQh|ryP MoDsV2FPT0WU
NCI-H292 MoW5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTVyLki3OVgh|ryP NXHGO25qW0GQR1XS
Sk-ChA-1  NIXucYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jVO|AvOjYkgKO1NEDPxE1? M3ztZlczKGh? MkTOTWM2OD15ND61OOKyOi53ON88US=> M13zc|I2PzR{NEiy
Mz-ChA-1 M2rkcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIraV|cxNjJ34pETOVAh|ryP M{XBVFczKGh? NWfLeIFqUUN3ME21OE46P8LzMz60Oe69VQ>? M2HpVFI2PzR{NEiy
Smo-WT MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13yNmlEPTEEoH;mJFE1yqCwTR?= MWOyOFI6OTFyNB?=
Smo-D473H  MnHpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFnsW2FKSzVywrDv[kA4NjIEoN88US=> NFzBNIMzPDJ7MUGwOC=>
K562 NIewXpFHfW6ldHnvckBCe3OjeR?= NHrVRpgyOCEQvF2= MYi3NkBp MV7y[YR2[2W|IITo[UBmgHC{ZYPzbY9vKG:oIFfsbVHDqA>? NGfZOYkzOzNzOUiyOC=>
TF-1 BCR-ABL M{W3ZmZ2dmO2aX;uJGF{e2G7 NHPZN4cyOCEQvF2= MlfpO|IhcA>? NFWzeXpz\WS3Y3XzJJRp\SCneIDy[ZN{cW:wIH;mJGdtcTIEoB?= NI\PUoIzOzNzOUiyOC=>

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
Fas / DR4 / DR5 / Cleaved PARP / Bcl-2 / Cleaved caspase-3 / PDGFRα; 

PubMed: 22087285     

Pancreatic CSCs were treated with GDC-0449 (0, 1, 5 and 10 µM) for 48 h. The expression of Fas, DR4/TRAIL-R1, DR5/TRAIL-R2, PARP cleavage, Bcl-2, and Caspase-3 by the Western blot analysis. β-Actin was used as a loading control.

p-GSK3β / GSK3β / p-Akt / Akt / Gli1; 

PubMed: 27143997     

Cells were pretreated with or without 30 μM GDC-0449 for 2 h before TMT treatment. After incubation with 3.75 μM TMT for another 24 h, the expression levels of proteins were determined through Western blot analysis.

Gli1 / SOX2 / OCT4; 

PubMed: 26418365     

The activation of Hedgehog pathways and CSC markers were tested by immunoblotting analysis in Hs578T and BT549 cells. β‐Actin was used as a loading control.

p53 / Cyclin D1 / p21; 

PubMed: 28195165     

GDC-0449 treatment affected the expression levels of cell cycle-related protein levels. U251 cells were treated with 0.1% DMSO or GDC-0449 at the indicated concentrations for 24 h. Cells were then harvested and examined using Western blot analysis with the indicated antibodies.

Bcl-2 / Bax; 

PubMed: 28195165     

GDC-0449 treatment affected the expression levels of cell cycle-related protein levels. U251 cells were treated with 0.1% DMSO or GDC-0449 at the indicated concentrations for 24 h. Cells were then harvested and examined using Western blot analysis with the indicated antibodies.

22087285 27143997 26418365 28195165
Gli1 / Gli2; 

PubMed: 22087285     

GDC-0449 inhibits expression of Gli1 and Gli2 in human pancreatic CSCs. The cells were seeded on fibronectin-coated coverslips and treated with GDC-0449 (10 µM) for 48 h. Subsequently, cells were fixed with 4% paraformaldehyde, blocked in 10% normal goat serum and stained with Gli1 and Gli2 primary antibodies (1∶100) for 16 h at 4°C and washed with PBS. Afterwards, cells were incubated with fluorescently labeled secondary antibody (1∶200) along with DAPI (1 mg/ml) for 1 h at room temperature and cells were mounted and visualized under a fluorescent microscope. For better visuality, the color of DAPI was changed from blue to red.

Growth inhibition assay
Cell viability; 

PubMed: 29042665     

GDC-0449 improves the anti-proliferation activity in NIH-3T3 cells but not in BxPC-3, Panc-1, MIAPaca-2 and SW1990 cells when cultured alone. The cytotoxicities of GDC-0449, Dox or Dox with GDC-0449 (5 μM or 10 μM) were measured by performing a 48-h MTT assay in BxPC-3 (A), Panc-1 (B), MIAPaca-2 (C), SW1990 (D) and NIH-3T3 (E) cells. Apoptosis rate was detected by flow cytometry (Annexin V staining) analysis after treatment with Dox (200 nM) with or without GDC-0449 for 24 h (F). Data are presented as the mean ± SD. *P < 0.05, **P < 0.01.

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]


Cell Research:[2]
- Collapse
  • 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.
    (Only for Reference)
Animal Research:[4]
- Collapse
  • Animal Models: Ptch(+/-) allograft model, D5123 and 1040830
  • Formulation: In 0.5% methyl-cellulose, 0.2% tween-80
  • Dosages: ~ 100 mg/kg
  • Administration: Orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 84 mg/mL (199.38 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.

* 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 Information

Molecular Weight 421.3


CAS No. 879085-55-9
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03610022 Recruiting Drug: Treatment with vismodegib Metastatic Basal Cell Carcinoma|Locally Advanced Basal Cell Carcinoma University Hospital Bordeaux September 3 2018 Phase 4
NCT03035188 Recruiting Drug: Vismodegib Basal Cell Carcinoma SRH Wald-Klinikum Gera GmbH January 2017 Phase 2
NCT02781389 Active not recruiting -- Basal Cell Carcinoma University Hospital Essen|OnkoDataMed GmbH April 29 2016 --
NCT02648048 Completed Drug: Pirfenidone|Drug: Vismodegib Idiopathic Pulmonary Fibrosis Hoffmann-La Roche January 15 2016 Phase 1
NCT02593760 Completed Other: Placebo|Drug: Ruxolitinib|Drug: Vismodegib Myelofibrosis Hoffmann-La Roche January 25 2016 Phase 1
NCT02366312 Completed Drug: vismodegib Keratocystic Odontogenic Tumor NYU College of Dentistry|Genentech Inc. October 27 2015 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID