Cat. No.: HY-10440

Vismodegib

(Synonyms: GDC-0449)

53 Cited Publications

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Based on 53 publication(s) in Google Scholar

Vismodegib (GDC-0449) is a BBB-permeable and orally active hedgehog pathway inhibitor with an IC₅₀ of 3 nM. Vismodegib also inhibits P-gp, ABCG2 with IC₅₀ values of 3.0 μM and 1.4 μM, respectively.

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Pureté: 99.90%
CAS No.: 879085-55-9
Formule: C₁₉H₁₄Cl₂N₂O₃S
Masse moléculaire:421.30

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Vismodegib Chemical Structure

CAS No.: 879085-55-9

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (53)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
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Activité biologique

Description

IC₅₀ & Target

IC50: 3 nM (hedgehog), 3.0 μM (P-gp), 1.4 μM (ABCG2)^[1]^[2]

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	>100 μM Compound: VIS; GDC-0449	Antiproliferation activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferation activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 32690258]
AN3-CA	IC₅₀	93 μM Compound: VIS; GDC-0449	Antiproliferation activity against human AN3CA cells assessed as reduction in cell viability incubated for 72 hr by MTT assay Antiproliferation activity against human AN3CA cells assessed as reduction in cell viability incubated for 72 hr by MTT assay	[PMID: 32690258]
BXPC-3	IC₅₀	47.95 μM Compound: 1; GDC-0449	Antiproliferative activity against human BxPC3 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human BxPC3 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 26820554]
C3H 10T1/2	EC₅₀	4.7 nM Compound: 1	Inhibition of SMO-mediated Hedgehog signaling pathway in mouse C3H10T1/2 cells assessed as reduction in sonic hedgehog-induced osteoblast differentiation by measuring alkaline phosphatase activity incubated for 72 hrs Inhibition of SMO-mediated Hedgehog signaling pathway in mouse C3H10T1/2 cells assessed as reduction in sonic hedgehog-induced osteoblast differentiation by measuring alkaline phosphatase activity incubated for 72 hrs	[PMID: 31862310]
C3H 10T1/2	IC₅₀	0.011 μM Compound: GDC-0449	Inhibition of SAG-induced differentiation of mouse mesenchymal pluripotent C3H10T1/2 cells to alkaline phosphatase positive oeseoblasts after 6 hrs Inhibition of SAG-induced differentiation of mouse mesenchymal pluripotent C3H10T1/2 cells to alkaline phosphatase positive oeseoblasts after 6 hrs	[PMID: 22268551]
C3H 10T1/2	IC₅₀	0.013 μM Compound: 31, GDC-0449	Inhibition of SHH in mouse C3H10T1/2 cells by Gli-luciferase reporter gene assay Inhibition of SHH in mouse C3H10T1/2 cells by Gli-luciferase reporter gene assay	[PMID: 19716296]
C3H 10T1/2	IC₅₀	0.017 μM Compound: Vismodegib	Inhibition of hedgehog signalling in mouse C3H10T1/2 cells assessed as reduction in Smo agonist SAG induced cell differentiation into alkaline phosphatase-positive osteoblasts using pNp substrate incubated for 72 hrs Inhibition of hedgehog signalling in mouse C3H10T1/2 cells assessed as reduction in Smo agonist SAG induced cell differentiation into alkaline phosphatase-positive osteoblasts using pNp substrate incubated for 72 hrs	10.1039/C5MD00092K
C3H 10T1/2	IC₅₀	5 nM Compound: GDC-0449	Inhibition of Smo in mouse C3H10T1/2 cells using human recombinant SHH assessed as effect on SMO/SHH transient transcriptional activation after 20 hrs by Gli-luciferase reporter assay Inhibition of Smo in mouse C3H10T1/2 cells using human recombinant SHH assessed as effect on SMO/SHH transient transcriptional activation after 20 hrs by Gli-luciferase reporter assay	[PMID: 24900436]
CCRF-CEM	IC₅₀	58 μM Compound: 17	Antiproliferative activity against human CEM cells incubated for 96 hrs by Coulter counter method Antiproliferative activity against human CEM cells incubated for 96 hrs by Coulter counter method	[PMID: 32686940]
Daoy	IC₅₀	0.086 μM Compound: 1, GDC-0449	Inhibition of Hedgehog signaling in human DaOY cells assessed as downregulation of Gli1 mRNA expression after 48 hrs by RT-PCR analysis Inhibition of Hedgehog signaling in human DaOY cells assessed as downregulation of Gli1 mRNA expression after 48 hrs by RT-PCR analysis	[PMID: 24900716]
HEK293	IC₅₀	0.0051 μM Compound: 54	Displacement of BODIPY-cyclopamine from human Smo expressed in HEK293 cells incubated for 3 hrs by fluorescence competitive displacement assay Displacement of BODIPY-cyclopamine from human Smo expressed in HEK293 cells incubated for 3 hrs by fluorescence competitive displacement assay	10.1039/C6MD00020G
HEK293	IC₅₀	0.006 μM Compound: Vismodegib	Displacement of boron-dipyrromethene-cyclopamine from human smoothened receptor expressed in HEK293 cells incubated for 4 hrs by hSMO-BC binding assay Displacement of boron-dipyrromethene-cyclopamine from human smoothened receptor expressed in HEK293 cells incubated for 4 hrs by hSMO-BC binding assay	10.1039/C5MD00092K
HEK293	IC₅₀	7 nM Compound: GDC-0449	Displacement of BODIPY-labelled cyclopamine from human Smo receptor expressed in HEK293 cells after 2 hrs by fluorescence microscopy Displacement of BODIPY-labelled cyclopamine from human Smo receptor expressed in HEK293 cells after 2 hrs by fluorescence microscopy	[PMID: 22268551]
HeLa	EC₅₀	0.002 μM Compound: 1	Displacement of BODIPY-labeled cyclopamine from mouse SMO transfected in human HeLa cells by competition binding assay Displacement of BODIPY-labeled cyclopamine from mouse SMO transfected in human HeLa cells by competition binding assay	[PMID: 31862310]
HeLa	EC₅₀	0.003 μM Compound: 1	Displacement of BODIPY-labeled cyclopamine from human SMO transfected in human HeLa cells by competition binding assay Displacement of BODIPY-labeled cyclopamine from human SMO transfected in human HeLa cells by competition binding assay	[PMID: 31862310]
HeLa	IC₅₀	61.7 μM Compound: VIS; GDC-0449	Antiproliferation activity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferation activity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 32690258]
HeLa	IC₅₀	64 μM Compound: 17	Antiproliferative activity against human HeLa cells incubated for 4 days by Coulter counter method Antiproliferative activity against human HeLa cells incubated for 4 days by Coulter counter method	[PMID: 32686940]
HMEC-1	IC₅₀	41 μM Compound: 17	Growth inhibition of HMEC-1 incubated for 4 days by Coulter counter method Growth inhibition of HMEC-1 incubated for 4 days by Coulter counter method	[PMID: 32686940]
HT-1080	IC₅₀	>100 μM Compound: GDC-0449; 1	Antiproliferative activity against human HT1080 cells after 72 hrs by sulforhodamine-B assay Antiproliferative activity against human HT1080 cells after 72 hrs by sulforhodamine-B assay	[PMID: 30099257]
HT-29	IC₅₀	1.08 μM Compound: Vismodegib	Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition after 48 hrs by MTT assay Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition after 48 hrs by MTT assay	10.1039/C5MD00092K
L1210	IC₅₀	49 μM Compound: 17	Antiproliferative activity against mouse L1210 cells incubated for 48 hrs by Coulter counter method Antiproliferative activity against mouse L1210 cells incubated for 48 hrs by Coulter counter method	[PMID: 32686940]
LS174T	IC₅₀	45.81 μM Compound: 1; GDC-0449	Antiproliferative activity against human LS174T cells after 72 hrs by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human LS174T cells after 72 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 26820554]
LS180	IC₅₀	45 μM Compound: GDC-0449; 1	Antiproliferative activity against human LS180 cells after 72 hrs by sulforhodamine-B assay Antiproliferative activity against human LS180 cells after 72 hrs by sulforhodamine-B assay	[PMID: 30099257]
MCF-10A	IC₅₀	89.5 μM Compound: VIS; GDC-0449	Cytotoxicity against human MCF10A cells assessed as cell viability incubated for 72 hrs measured by MTT assay Cytotoxicity against human MCF10A cells assessed as cell viability incubated for 72 hrs measured by MTT assay	[PMID: 32690258]
MCF7	IC₅₀	>100 μM Compound: VIS; GDC-0449	Antiproliferation activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferation activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 32690258]
MCF7	IC₅₀	>50 μM Compound: Vismodegib	Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 29107429]
MDA-MB-231	IC₅₀	>100 μM Compound: VIS; GDC-0449	Antiproliferation activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs measured after 4 hrs by MTT assay Antiproliferation activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs measured after 4 hrs by MTT assay	[PMID: 32690258]
MDA-MB-231	IC₅₀	>50 μM Compound: Vismodegib	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 29107429]
MDA-MB-468	IC₅₀	79 μM Compound: VIS; GDC-0449	Antiproliferation activity against human MDA-MB-468 cells assessed as reduction in cell viability incubated for 72 hr by MTT assay Antiproliferation activity against human MDA-MB-468 cells assessed as reduction in cell viability incubated for 72 hr by MTT assay	[PMID: 32690258]
Medulloblastoma cell	IC₅₀	30.4 nM Compound: 1; GDC-0449	Antiproliferative activity against Ptch+/- and p53-/- mouse medulloblastoma cells after 36 hrs by Brdu incorporation assay Antiproliferative activity against Ptch+/- and p53-/- mouse medulloblastoma cells after 36 hrs by Brdu incorporation assay	[PMID: 28688278]
Medulloblastoma cell	IC₅₀	4.7 nM Compound: GDC-0449	Antiproliferative activity against mouse Ptch+/- medulloblastoma cells assessed as inhibition of cell growth incubated for 36 hrs by CCK-8 assay Antiproliferative activity against mouse Ptch+/- medulloblastoma cells assessed as inhibition of cell growth incubated for 36 hrs by CCK-8 assay	[PMID: 30939349]
MGC-803	IC₅₀	2.39 μM Compound: Vismodegib	Antiproliferative activity against human MGC803 cells assessed as cell growth inhibition after 48 hrs by MTT assay Antiproliferative activity against human MGC803 cells assessed as cell growth inhibition after 48 hrs by MTT assay	10.1039/C5MD00092K
NIH3T3	IC₅₀	0.023 μM Compound: GDC-0449	Inhibition of Smo receptor (unknown origin) expressed in NIH3T3 cells assessed as inhibition of Smo agonist SAG-induced GRE activation after 30 hrs by luciferase reporter gene assay Inhibition of Smo receptor (unknown origin) expressed in NIH3T3 cells assessed as inhibition of Smo agonist SAG-induced GRE activation after 30 hrs by luciferase reporter gene assay	[PMID: 24726807]
NIH3T3	IC₅₀	0.025 μM Compound: 54	Inhibition of Hh receptor (unknown origin) expressed in SAG-stimulated mouse NIH3T3 cells incubated for 24 hrs by Gli-luciferase reporter gene assay Inhibition of Hh receptor (unknown origin) expressed in SAG-stimulated mouse NIH3T3 cells incubated for 24 hrs by Gli-luciferase reporter gene assay	10.1039/C6MD00020G
NIH3T3	IC₅₀	7.17 nM Compound: GDC-0449	Inhibition of hedgehog receptor signaling pathway in mouse NIH3T3 cells transfected with Gli-reporter gene by luciferase reporter gene assay Inhibition of hedgehog receptor signaling pathway in mouse NIH3T3 cells transfected with Gli-reporter gene by luciferase reporter gene assay	[PMID: 24923765]
NIH3T3	IC₅₀	7.2 nM Compound: 1; GDC-0449	Inhibition of Sonic-induced hedgehog signalling in mouse NIH3T3 cells after 48 hrs by Gli-luciferase reporter assay Inhibition of Sonic-induced hedgehog signalling in mouse NIH3T3 cells after 48 hrs by Gli-luciferase reporter assay	[PMID: 26820554]
NIH3T3	IC₅₀	7.2 nM Compound: 1; GDC-0449	Inhibition of hedgehog signalling in mouse NIH3T3 cells stably transfected with Gli-luciferase construct incubated for 48 hrs by dual luciferase reporter gene assay Inhibition of hedgehog signalling in mouse NIH3T3 cells stably transfected with Gli-luciferase construct incubated for 48 hrs by dual luciferase reporter gene assay	[PMID: 26827136]
NIH3T3	IC₅₀	7.2 nM Compound: GDC, GDC-0449	Inhibition of hedgehog signaling pathway in mouse NIH/3T3 cells by Gli1-luciferase reporter gene assay Inhibition of hedgehog signaling pathway in mouse NIH/3T3 cells by Gli1-luciferase reporter gene assay	[PMID: 24405704]
NIH3T3	IC₅₀	7.2 nM Compound: GDC-0449	Inhibition of hedgehog signaling pathway in mouse NIH/3T3 cells after 48 hrs by Gli-luciferase reporter gene assay Inhibition of hedgehog signaling pathway in mouse NIH/3T3 cells after 48 hrs by Gli-luciferase reporter gene assay	[PMID: 24486203]
NIH3T3	IC₅₀	7.2 nM Compound: GDC-0449, vismodegib	Inhibition of SHH signaling pathway in mouse NIH3T3 cells measured after 48 hrs by Gli-luciferase reporter assay Inhibition of SHH signaling pathway in mouse NIH3T3 cells measured after 48 hrs by Gli-luciferase reporter assay	[PMID: 24176396]
PC-3	IC₅₀	>50 μM Compound: Vismodegib	Cytotoxicity against human PC3 cells after 72 hrs by MTT assay Cytotoxicity against human PC3 cells after 72 hrs by MTT assay	[PMID: 29107429]
PC-3	IC₅₀	66.78 μM Compound: 1; GDC-0449	Antiproliferative activity against human PC3 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human PC3 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 26820554]
Shh Light II	IC₅₀	0.007 μM Compound: GDC-0449	Inhibition of Smo-mediated Hh signaling in human Shh-light2 cells by luciferase reporter gene assay Inhibition of Smo-mediated Hh signaling in human Shh-light2 cells by luciferase reporter gene assay	[PMID: 22268551]
Shh Light II	IC₅₀	1.5 nM Compound: GDC-0449	Antagonist activity at Smo in mouse Shh-Light 2 cells assessed as inhibition of Shh-induced Gli1-reporter activity after 2 days by dual-luciferase reporter gene method Antagonist activity at Smo in mouse Shh-Light 2 cells assessed as inhibition of Shh-induced Gli1-reporter activity after 2 days by dual-luciferase reporter gene method	[PMID: 23063522]
Shh Light II	IC₅₀	3 nM Compound: 101, GDC-0449	Inhibition of SHH in mouse Shh Light2 cells by GLI-responsive firefly luciferase reporter gene assay Inhibition of SHH in mouse Shh Light2 cells by GLI-responsive firefly luciferase reporter gene assay	[PMID: 19309080]
Shh Light II	IC₅₀	33 nM Compound: GDC-0449	Antagonist activity at smoothened (unknown origin) expressed in mouse Shh Light2 cells co-expressing Gli-dependent reporter gene assessed as inhibition of Hh signaling by dual luciferase reporter gene assay Antagonist activity at smoothened (unknown origin) expressed in mouse Shh Light2 cells co-expressing Gli-dependent reporter gene assessed as inhibition of Hh signaling by dual luciferase reporter gene assay	[PMID: 24491459]
SW-620	IC₅₀	10.92 μM Compound: Vismodegib	Antiproliferative activity against human SW620 cells assessed as cell growth inhibition after 48 hrs by MTT assay Antiproliferative activity against human SW620 cells assessed as cell growth inhibition after 48 hrs by MTT assay	10.1039/C5MD00092K
T47D	IC₅₀	>100 μM Compound: VIS; GDC-0449	Antiproliferation activity against human T47D cells assessed as reduction in cell viability incubated for 72 hr by MTT assay Antiproliferation activity against human T47D cells assessed as reduction in cell viability incubated for 72 hr by MTT assay	[PMID: 32690258]
T47D	IC₅₀	41.34 μM Compound: Vismodegib	Cytotoxicity against human T47D cells after 72 hrs by MTT assay Cytotoxicity against human T47D cells after 72 hrs by MTT assay	[PMID: 29107429]
U-251	IC₅₀	>100 μM Compound: VIS; GDC-0449	Antiproliferation activity against human U251 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferation activity against human U251 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 32690258]
U2OS	IC₅₀	74 nM Compound: GDC-0449	Displacement of BODIPY-Cyclopamine from human HA-tagged Smo receptor expressed in human U2OS cells at 1 to 10000 nM incubated for 2 hrs by DAPI staining based fluorescence microscopic method Displacement of BODIPY-Cyclopamine from human HA-tagged Smo receptor expressed in human U2OS cells at 1 to 10000 nM incubated for 2 hrs by DAPI staining based fluorescence microscopic method	[PMID: 30939349]

In Vitro

Vismodegib (HhAntag691) is an ABCG2 inhibitor and can increase the effective intracellular concentration of NSC 279836, another ABCG2 substrate, through blocking its export in HEK293 cells. Vismodegib (HhAntag691, 10 μM), resensitizes MDCKII/Pgp cells and MDCKII/MRP1 cells to NSC757 treatment^[2].
Vismodegib (25 μM or 50 μM) concentration-dependently inhibits HCC and H1339 cells^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Vismodegib (0.3 to 75 mg/kg, p.o.) is highly efficacious in medulloblastoma allograft tumors. Vismodegib (> 46 mg/kg, p.o.) causes growth delay in patient-derived colorectal xenografts^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 879085-55-9
Appearance Solid
Masse moléculaire 421.30
Formule C₁₉H₁₄Cl₂N₂O₃S
Color Off-white to light yellow
SMILES

O=C(C1=CC=C(C=C1Cl)S(=O)(C)=O)NC2=CC=C(C(C3=NC=CC=C3)=C2)Cl
Synonyms

GDC-0449
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (53)

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Journal Impact Factor

Genes Dis

IRE1α regulates the PTHrP-IHH feedback loop to orchestrate chondrocyte hypertrophy and cartilage mineralization. [Abstract]

2022 Dec 29;11(1):464-478. PMID: 37588212
J Exp Clin Cancer Res

SCP2-mediated cholesterol membrane trafficking promotes the growth of pituitary adenomas via Hedgehog signaling activation. [Abstract]

2019 Sep 13;38(1):404. PMID: 31519191
Adv Sci (Weinh)

Single-Cell RNA-Sequencing Provides Insight into Skeletal Muscle Evolution during the Selection of Muscle Characteristics. [Abstract]

2023 Dec;10(35):e2305080. PMID: 37870215
Biomaterials

Dually fibronectin/CD44-mediated nanoparticles targeted disrupt the Golgi apparatus and inhibit the hedgehog signaling in activated hepatic stellate cells to alleviate liver fibrosis. [Abstract]

2023 Oct:301:122232. PMID: 37418856
Neuro Oncol

Intraventricular SHH inhibition proves efficient in SHH medulloblastoma mouse model and prevents systemic side effects. [Abstract]

2024 Apr 5;26(4):609-622. PMID: 37767814
J Control Release

An integrin-based nanoparticle that targets activated hepatic stellate cells and alleviates liver fibrosis. [Abstract]

2019 Jun 10:303:77-90. PMID: 31004666
Cancer Lett

Cynanbungeigenin C and D, a pair of novel epimers from Cynanchum bungei, suppress hedgehog pathway-dependent medulloblastoma by blocking signaling at the level of Gli. [Abstract]

2018 Apr 28:420:195-207. PMID: 29425683

Vismodegib purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2018 Apr 28:420:195-207. [Abstract]

Shh-Light 2 cells are transfected with Gli1 or Gli2 plasmids and the expression of proteins are analyzed by Western blot. Positive control JQ1, CBC and CBD inhibit Gli1 and Gli2 overexpression induced Gli luciferase activity, GDC-0499 and GANT61 have no effects.
Acta Pharmacol Sin

Sonic Hedgehog-Gli1 signaling promotes microglial activation via the IKKβ/NF-κB pathway. [Abstract]

2026 Mar 11. PMID: 41813972
Biomater Res

Tryptamine-Functionalized Lipid Nanocarriers Co-delivering SMO/BRD4 Inhibitors for Synergistic Medulloblastoma Therapy. [Abstract]

2025 Aug 8:29:0237. PMID: 40785845
Oncogene

Nuclear receptor coactivator SRC-1 promotes colorectal cancer progression through enhancing GLI2-mediated Hedgehog signaling. [Abstract]

2022 May;41(20):2846-2859. PMID: 35418691
Oncogene

Genetic landscape and ligand-dependent activation of sonic hedgehog-Gli1 signaling in chordomas: a novel therapeutic target. [Abstract]

2020 Jun;39(24):4711-4727. PMID: 32404987
Oncogene

Inflammation-induced JMJD2D promotes colitis recovery and colon tumorigenesis by activating Hedgehog signaling. [Abstract]

2020 Apr;39(16):3336-3353. PMID: 32094404
EMBO Mol Med

circ-EGFR is a predictor of response to Cetuximab and a potential target in colorectal cancer. [Abstract]

2025 Dec;17(12):3525-3554. PMID: 41214390
J Genet Genomics

Reduced Smoothened level rescues Aβ-induced memory deficits and neuronal inflammation in animal models of Alzheimer's disease. [Abstract]

2018 May 20;45(5):237-246. PMID: 29807798

Vismodegib purchased from MedChemExpress. Usage Cited in: J Genet Genomics. 2018 May 20;45(5):237-246. [Abstract]

Drug-feeding scheme (upper panel). Memory rescuing effects through treatment with LDE225 (LDE) or Vismodegib (VIS) at 20 mg/kg for 7.5-m-old and 15-m-old mice (lower panel, n=7 for each group).
ACS Appl Mater Interfaces

Structure-Selective Polydopamine Coating on Drug Nanoparticles. [Abstract]

2026 Jan 25. PMID: 41582522
Sci Signal

The kinase PLK1 promotes Hedgehog signaling-dependent resistance to the antiandrogen enzalutamide in metastatic prostate cancer. [Abstract]

2025 Mar 18;18(878):eadi5174. PMID: 40100956
Drug Deliv Transl Res

Enhanced skin delivery of vismodegib by microneedle treatment. [Abstract]

2015 Aug;5(4):407-23. PMID: 26069156
Life Sci

Intervention of epithelial mesenchymal transition against colon cancer cell growth and metastasis based on SOX21/POU4F2/Hedgehog signaling axis. [Abstract]

2024 Sep 1:352:122905. PMID: 38992573
Biomed J

Repurposing old drugs as antiviral agents for coronaviruses. [Abstract]

2020 Aug;43(4):368-374. PMID: 32563698
Int J Pharm

Fractional ablative laser-enhanced transdermal delivery of vismodegib: systematic evaluation of microporation parameters and permeation kinetics. [Abstract]

2026 Mar 2:126737. PMID: 41780611
Oncogenesis

Cigarette smoke stimulates the stemness of renal cancer stem cells via Sonic Hedgehog pathway. [Abstract]

2018 Mar 13;7(3):24. PMID: 29540668

Vismodegib purchased from MedChemExpress. Usage Cited in: Oncogenesis. 2018 Mar 13;7(3):24. [Abstract]

786-O and ACHN tumorspheres are treated with 0.1% CSE with/without 10 mM Vismodegib for 5 days. Western blotting analysis of SHH pathway proteins.
Cell Rep Methods

RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]

2023 Oct 23;3(10):100599. PMID: 37797618
RSC Pharm

2025 Oct 9.
Front Cell Dev Biol

Apatinib Suppresses Gastric Cancer Stem Cells Properties by Inhibiting the Sonic Hedgehog Pathway. [Abstract]

2021 Jul 19:9:679806. PMID: 34350176
Eur J Pharm Sci

Impact of gamma irradiation and ethylene oxide sterilisation on the stability of crystalline and amorphous drug solids. [Abstract]

2026 Jun 6:224:107572. PMID: 42250781
Biochim Biophys Acta Mol Basis Dis

YAP/Aurora A-mediated ciliogenesis regulates ionizing radiation-induced senescence via Hedgehog pathway in tumor cells. [Abstract]

2024 Feb 10;1870(4):167062. PMID: 38342416
Mol Pharm

Glassy Drug Microneedle Array Design: Drug Glass-Forming Ability and Stability. [Abstract]

2025 Mar 3;22(3):1373-1383. PMID: 39957277
FASEB J

HOXB4 Promotes Bladder Cancer Progression in Part Through Transcriptional Activation of Smoothened. [Abstract]

2026 Jan 15;40(1):e71388. PMID: 41502296
Drug Dev Res

Panaxadiol Attenuates Brain Damage by Inhibiting Ferroptosis in a Rat Model of Cerebral Hemorrhage. [Abstract]

2025 Apr;86(2):e70079. PMID: 40117294
Development

Axin1 regulates tooth root development by inhibiting AKT1-mTORC1 activation and Shh translation in Hertwig's epithelial root sheath. [Abstract]

2024 Nov 1;151(21):dev202899. PMID: 39344774
Mol Carcinog

Diallyl trisulfide inhibits gastric cancer stem cell properties through ΔNp63/sonic hedgehog pathway. [Abstract]

2023 Nov;62(11):1673-1685. PMID: 37477518
Bioorg Med Chem

Steroidal alkaloids isolated from Veratrum grandiflorum Loes. as novel Smoothened inhibitors with anti-proliferation effects on DAOY medulloblastoma cells. [Abstract]

2021 Jun 1:39:116166. PMID: 33910157
Am J Physiol Gastrointest Liver Physiol

Inhibition of hedgehog signaling ameliorates severity of chronic pancreatitis in experimental mouse models. [Abstract]

2025 Apr 1;328(4):G342-G363. PMID: 39499252
Cell Biochem Biophys

Combination of Vismodegib and Paclitaxel Enhances Cytotoxicity via Bak-mediated Mitochondrial Damage in EGFR-Mutant Non-Small Cell Lung Cancer Cells. [Abstract]

2024 Dec;82(4):3499-3506. PMID: 39030332
Prostate

SEMA3C induces androgen synthesis in prostatic stromal cells through paracrine signaling. [Abstract]

2021 May;81(6):309-317. PMID: 33503318
Purinergic Signal

Antagonism of the ATP-gated P2X7 receptor inhibits the proliferation of hepatocellular carcinoma cells. [Abstract]

2024 Nov 16. PMID: 39549156
Arch Oral Biol

GDC-0449 suppresses odontogenic keratocyst aggressiveness in fibroblasts by upregulating SPARC via Hedgehog pathway inhibition. [Abstract]

2025 Aug 13:179:106374. PMID: 40840062
Oncol Lett

Sonic hedgehog pathway mediates genistein inhibition of renal cancer stem cells. [Abstract]

2019 Sep;18(3):3081-3091. PMID: 31452785
Parasitol Int

Possible antifibrotic effect of GDC-0449 (Vismodegib), a hedgehog-pathway inhibitor, in mice model of Schistosoma-induced liver fibrosis. [Abstract]

2017 Oct;66(5):545-554. PMID: 28408356
J Biophotonics

Regeneration of taste through sonic hedgehog upregulation by photobiomodulation. [Abstract]

2023 Nov;16(11):e202300043. PMID: 37483112
Hematology

SPRY1 promotes cell proliferation and inhibits apoptosis by activating Hedgehog pathway in acute myeloid leukemia. [Abstract]

2022 Dec;27(1):1-10. PMID: 34957932
Anticancer Drugs

Sonic hedgehog and Wnt/β-catenin pathways mediate curcumin inhibition of breast cancer stem cells. [Abstract]

2018 Mar;29(3):208-215. PMID: 29356693

Vismodegib purchased from MedChemExpress. Usage Cited in: Anticancer Drugs. 2018 Mar;29(3):208-215. [Abstract]

SUM159 sphereforming cells are treated with 15 μM XAV-939 for 7 days, and the protein expression levels of breast cancer stem cells (CSCs) markers are detected by western blotting.

Vismodegib purchased from MedChemExpress. Usage Cited in: Anticancer Drugs. 2018 Mar;29(3):208-215. [Abstract]

SUM159 sphere-forming cells are treated with Vismodegib (15 μM), a Smoothened (Smo) inhibitor for 7 days, and the protein expression levels of breast cancer stem cells (CSCs) play markers are detected by western blotting.
Dev Neurobiol

Sonic hedgehog antagonists reduce size and alter patterning of the frog inner ear. [Abstract]

2017 Dec;77(12):1385-1400. PMID: 29030893

Vismodegib purchased from MedChemExpress. Usage Cited in: Dev Neurobiol. 2017 Dec;77(12):1385-1400. [Abstract]

Reducing Shh signaling through Vismodegib treatment in Xenopus results in a significant rostral expansion of hypaxial muscle fibers.
Cell Press Blue

2026 Apr 22.
Res Sq

2026 Jan 9.
Biomed Pharmacother

Drug target proteome profiling identifies HES1-driven mitotic catastrophe in ovarian serous carcinoma. [Abstract]

2025 Dec:193:118716. PMID: 41202420
SSRN

2025 Jul 25.
SSRN

2023 Nov 14.
Friedrich-Alexander University Erlangen-Nuremberg

2023 May 2.
Research Square Preprint

2022 Jan.
Research Square Preprint

2020 Nov.
bioRxiv

2019 Mar.
Patent

US20180263995A1.

Solvant et solubilité

In Vitro:

DMSO : 50 mg/mL (118.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 3.33 mg/mL (7.90 mM; ultrasonic and warming and heat to 60°C)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3736 mL

11.8680 mL

23.7361 mL

5 mM

0.4747 mL

2.3736 mL

4.7472 mL

10 mM

0.2374 mL

1.1868 mL

2.3736 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.93 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (5.93 mM); Suspended solution; Need ultrasonic and warming

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.93 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocole

Cell Assay^[2]

When MTT assay is performed, an MTT reagent is added to each well to a final concentration of 150 µg/mL, and the cells are incubated for 1 to 2 hours at 37°C. The medium is then replaced with DMSO to dissolve the reaction product. Absorbance at 570 nm is quantified using a spectra MAX 340pc plate reader. For the XTT assay, 1 mg/mL XTT is mixed with 0.025 mM PMS, and 50 µL of the mixture is added to each well and incubated for 4 hours at 37°C. After the plates are mixed on a plate shaker, absorbance at 450 nm is measured. All results are normalized to a percentage of absorbance obtained in controls.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[2]

Tumor-bearing mice are distributed into tumor volume-matched cohorts when the tumors reache between 200 and 350 mm³. The vismodegib-resistant medulloblastoma allograft, sg274, is developed by intermittent suboptimal dosing of a Ptch^+/−, p53^−/−medulloblastoma allograft. Vismodegib is formulated as a suspension in 0.5% methyl-cellulose, 0.2% tween-80 (MCT), and is administered orally. Tumor volumes are determined using digital calipers using the formula (L×W×W)/2. Tumor growth inhibition (%TGI) is calculated as the percentage of the area under the fitted curve (AUC) for the respective dose group per day in relation to the vehicle, such that %TGI=100×1-(AUCtreatment/day)/(AUCvehicle/day).

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (281 KB)
SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Scales SJ, et al. Mechanisms of Hedgehog pathway activation in cancer and implications for therapy. Trends Pharmacol Sci. 2009, 30(6), 303-312. [Content Brief]

[2]. Zhang Y, et al. Hedgehog pathway inhibitor HhAntag691 is a potent inhibitor of ABCG2/BCRP and ABCB1/Pgp. Neoplasia. 2009, 11(1), 96-101. [Content Brief]

[3]. Tian F, et al. The hedgehog pathway inhibitor GDC-0449 alters intracellular Ca²⁺ homeostasis and inhibits cell growth in NSC 119875-resistant lung cancer cells. Anticancer Res. 2012, 32(1), 89-94. [Content Brief]

[4]. Wong H, et al. Pharmacokinetic-pharmacodynamic analysis of vismodegib in preclinical models of mutational and ligand-dependent Hedgehog pathway activation. Clin Cancer Res. 2011, 17(14), 4682-4692. [Content Brief]

[5]. Elhenawy AA, et al. Possible antifibrotic effect of GDC-0449 (Vismodegib), a hedgehog-pathway inhibitor, in mice model of Schistosoma-induced liver fibrosis. Parasitol Int. 2017 Oct;66(5):545-554. [Content Brief]

[6]. Ma W, et al. Reduced Smoothened level rescued Aβ-induced memory deficits and neuronal inflammation in animal models of Alzheimer's disease. J Genet Genomics. 2018 May 20;45(5):237-246. [Content Brief]

[7]. Xing G, et al. Astrocytic Sonic Hedgehog Alleviates Intracerebral Hemorrhagic Brain Injury via Modulation of Blood-Brain Barrier Integrity. Front Cell Neurosci. 2020 Dec 3;14:575690. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
Ethanol / DMSO	1 mM	2.3736 mL	11.8680 mL	23.7361 mL	59.3401 mL
Ethanol / DMSO	5 mM	0.4747 mL	2.3736 mL	4.7472 mL	11.8680 mL
DMSO	10 mM	0.2374 mL	1.1868 mL	2.3736 mL	5.9340 mL
	15 mM	0.1582 mL	0.7912 mL	1.5824 mL	3.9560 mL
	20 mM	0.1187 mL	0.5934 mL	1.1868 mL	2.9670 mL
	25 mM	0.0949 mL	0.4747 mL	0.9494 mL	2.3736 mL
	30 mM	0.0791 mL	0.3956 mL	0.7912 mL	1.9780 mL
	40 mM	0.0593 mL	0.2967 mL	0.5934 mL	1.4835 mL
	50 mM	0.0475 mL	0.2374 mL	0.4747 mL	1.1868 mL
	60 mM	0.0396 mL	0.1978 mL	0.3956 mL	0.9890 mL
	80 mM	0.0297 mL	0.1484 mL	0.2967 mL	0.7418 mL
	100 mM	0.0237 mL	0.1187 mL	0.2374 mL	0.5934 mL

Keywords

Vismodegib

53 Cited Publications

100 mg Obtenir un devis

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Vismodegib

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Publications Citing Use of MedChemExpress (MCE) Vismodegib

Activité biologique

Chemical Information

Publications (53)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Vismodegib Related Classifications

HY-10440 Related Classifications