Vismodegib (Synonyms: 维莫德吉; GDC-0449)

目录号: HY-10440 纯度: 99.95%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Vismodegib (GDC-0449) 是一种具有口服活性的 hedgehog 抑制剂，IC₅₀ 值为 3 nM；还可抑制 P-gp 和 ABCG2 的活性，IC₅₀ 值分别为 3.0 μM 和 1.4 μM。

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Vismodegib Chemical Structure

CAS No. : 879085-55-9

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥770	In-stock
5 mg	￥700	In-stock
10 mg	￥1080	In-stock
50 mg	￥2727	In-stock
100 mg	￥3972	In-stock
200 mg	￥5000	In-stock
500 mg		询价
1 g		询价

or 大包装询价

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Customer Review

Other Forms of Vismodegib:

Vismodegib (Standard) 询价

MCE 顾客使用本产品发表的 35 篇科研文献

: Vismodegib purchased from MCE. 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.

: Vismodegib purchased from MCE. 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.

: Vismodegib purchased from MCE. 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).

: Vismodegib purchased from MCE. 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 MCE. 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.

: Vismodegib purchased from MCE. 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.

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Vismodegib (GDC-0449) is an 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^[1]^[2].

IC₅₀ & Target

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

细胞效力
(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	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	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	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 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: 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: 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]
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]
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]

体外研究
(In Vitro)

Vismodegib (HhAntag691) 是一种 ABCG2 抑制剂，可通过阻断 HEK293 细胞中 NSC 279836 (另一种 ABCG2 底物) 的输出来增加其有效细胞内浓度。Vismodegib (HhAntag691，10 μM)，使 MDCKII/Pgp 细胞和 MDCKII/MRP1 细胞对 NSC757 处理重新敏感^[2]。
Vismodegib (25 μM 或 50 μM) 浓度依赖性地抑制 HCC 和 H1339 细胞^[3]。

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

体内研究
(In Vivo)

Vismodegib (0.3 to 75 mg/kg，po) 在髓母细胞瘤同种异体移植肿瘤中非常有效。Vismodegib (> 46 mg/kg，口服) 导致患者来源的结直肠异种移植物生长延迟^[4]。

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

Clinical Trial

分子量

421.30

Formula

C₁₉H₁₄Cl₂N₂O₃S

CAS 号

879085-55-9

性状

固体

颜色

Off-white to light yellow

中文名称

维莫德吉

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

溶解性数据

细胞实验：

DMSO 中的溶解度 : 50 mg/mL (118.68 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

Ethanol 中的溶解度 : 3.33 mg/mL (7.90 mM; 超声助溶 (<60°C))

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3736 mL	11.8681 mL	23.7362 mL
5 mM	0.4747 mL	2.3736 mL	4.7472 mL
10 mM	0.2374 mL	1.1868 mL	2.3736 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

摩尔计算器
稀释计算器

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.93 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.93 mM); 悬浊液; 超声加热助溶

此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.93 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.97%

选择批次：

Data Sheet (642 KB) SDS (419 KB)

COA (194 KB) HNMR (218 KB) LCMS (139 KB) 元素分析报告 (210 KB)

产品使用指南 (1538 KB)

参考文献

[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]

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. 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). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[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]

Vismodegib 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

Ethanol / DMSO	1 mM	2.3736 mL	11.8681 mL	23.7362 mL	59.3406 mL
Ethanol / DMSO	5 mM	0.4747 mL	2.3736 mL	4.7472 mL	11.8681 mL
DMSO	10 mM	0.2374 mL	1.1868 mL	2.3736 mL	5.9341 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

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Vismodegib879085-55-9GDC-0449维莫德吉GDC0449GDC 0449HedgehogAutophagyInhibitorinhibitorinhibit

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Vismodegib (Synonyms: 维莫德吉; GDC-0449)

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MCE 顾客使用本产品发表的 35 篇科研文献

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Vismodegib (Synonyms: 维莫德吉; GDC-0449)

Customer Review

Other Forms of Vismodegib:

Vismodegib 相关抗体

MCE 顾客使用本产品发表的 35 篇科研文献

Vismodegib 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

Vismodegib 相关抗体:

摩尔计算器

稀释计算器

Vismodegib 相关分类

完整储备液配制表

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