Reagenti e strumenti per immunologia, biologia cellulare e biologia molecolare

Adavosertib [955365-80-7]

Stampa

Cat# HY-10993-5mg

Size : 5mg

Marca : MedChemExpress

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Description

Adavosertib (AZD-1775; MK-1775) is a potent Wee1 inhibitor with an IC₅₀ of 5.2 nM.

IC₅₀ & Target

IC50: 5.2 nM (Wee1)

Cellular Effect

Cell Line	Type	Value	Description	References
A-427	IC₅₀	158 nM Compound: 1; AZD1775	Antiproliferative activity against human A-427 cells assessed as cell growth inhibition measured after 7 days by alamar blue assay Antiproliferative activity against human A-427 cells assessed as cell growth inhibition measured after 7 days by alamar blue assay	[PMID: 37197456]
A-427	IC₅₀	311 nM Compound: AZD1775	Antiproliferative activity against human A-427 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human A-427 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 38847373]
A-427	IC₅₀	78 nM Compound: AZD1775	Antiproliferative activity against human A-427 cells assessed as reduction in cell viability after 3 days by CellTiter-Glo assay Antiproliferative activity against human A-427 cells assessed as reduction in cell viability after 3 days by CellTiter-Glo assay	[PMID: 34423975]
A498	IC₅₀	215.5 nM Compound: AZD1775	Antiproliferative activity against human A498 cells assessed as cell growth inhibition measured after 72 hrs by SRB Assay Antiproliferative activity against human A498 cells assessed as cell growth inhibition measured after 72 hrs by SRB Assay	[PMID: 36170799]
BT-549	IC₅₀	0.49 μM Compound: 1; AZD1775	Antiproliferative activity against human BT-549 cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay Antiproliferative activity against human BT-549 cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay	[PMID: 35231578]
Daoy	IC₅₀	150 nM Compound: Adavosertib	Antiproliferative activity against human Daoy cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTS assay Antiproliferative activity against human Daoy cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTS assay	[PMID: 33636537]
HEK-293T	IC₅₀	0.29 μM Compound: MK-1775	Antiproliferative activity against HEK293T cells measured after 72 hrs by CellTiter-Blue assay Antiproliferative activity against HEK293T cells measured after 72 hrs by CellTiter-Blue assay	[PMID: 28792760]
LNCaP	IC₅₀	0.5 μM Compound: 1; AZD1775	Antiproliferative activity against human LNCaP cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay Antiproliferative activity against human LNCaP cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay	[PMID: 35231578]
LoVo	IC₅₀	328 nM Compound: AZD1775	Antiproliferative activity against human LoVo cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method Antiproliferative activity against human LoVo cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method	[PMID: 38847373]
MCF7	IC₅₀	1.1 μM Compound: 1; AZD1775	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay	[PMID: 35231578]
MDA-MB-231	IC₅₀	0.26 μM Compound: MK-1775	Antiproliferative activity against human MDA-MB-231 cells measured after 72 hrs by CellTiter-Blue assay Antiproliferative activity against human MDA-MB-231 cells measured after 72 hrs by CellTiter-Blue assay	[PMID: 28792760]
MM1.S	IC₅₀	0.31 μM Compound: MK-1775	Antiproliferative activity against human MM1S cells measured after 72 hrs by CellTiter-Blue assay Antiproliferative activity against human MM1S cells measured after 72 hrs by CellTiter-Blue assay	[PMID: 28792760]
MOLT-4	IC₅₀	800 nM Compound: AZD1775	Antiproliferative activity against human MOLT-4 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo Luminescent assay Antiproliferative activity against human MOLT-4 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo Luminescent assay	[PMID: 38663873]
MV4-11	IC₅₀	132.6 nM Compound: AZD1775	Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition measured after 72 hrs by SRB Assay Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition measured after 72 hrs by SRB Assay	[PMID: 36170799]
MV4-11	IC₅₀	95 nM Compound: AZD1775	Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by Celltiter-glo assay Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by Celltiter-glo assay	[PMID: 37167712]
Multiple myeloma cancer stem cell	IC₅₀	310 nM Compound: 17	Cytotoxicity against human Myeloma-stem like cells Cytotoxicity against human Myeloma-stem like cells	[PMID: 34974338]
NCI-H1299	IC₅₀	0.2837 nM Compound: AZD-1775; MK-1775	Inhibition of cell proliferation in human NCI-H1299 cells incubated for 3 days by MTT assay Inhibition of cell proliferation in human NCI-H1299 cells incubated for 3 days by MTT assay	[PMID: 35051747]
NCI-H1299	IC₅₀	104 nM Compound: AZD1775	Antiproliferative activity against human NCI-H1299 cells assessed as cell growth inhibition incubated for 3 days by CellTiter-Glo Luminescent assay Antiproliferative activity against human NCI-H1299 cells assessed as cell growth inhibition incubated for 3 days by CellTiter-Glo Luminescent assay	[PMID: 36075370]
NCI-H23	IC₅₀	122 nM Compound: AZD1775	Antiproliferative activity against human NCI-H23 cells assessed as reduction in cell viability after 4 days by CellTiter-Glo assay Antiproliferative activity against human NCI-H23 cells assessed as reduction in cell viability after 4 days by CellTiter-Glo assay	[PMID: 34423975]
NCI-H23	IC₅₀	175 nM Compound: 1; AZD1775	Antiproliferative activity against human NCI-H23 cells assessed as cell growth inhibition measured after 7 days by alamar blue assay Antiproliferative activity against human NCI-H23 cells assessed as cell growth inhibition measured after 7 days by alamar blue assay	[PMID: 37197456]
PC-3	IC₅₀	8 μM Compound: 1; AZD1775	Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay	[PMID: 35231578]
SUM149PT	IC₅₀	536.2 nM Compound: AZD1775	Antiproliferative activity against human SUM149PT cells assessed as cell growth inhibition measured after 72 hrs by SRB Assay Antiproliferative activity against human SUM149PT cells assessed as cell growth inhibition measured after 72 hrs by SRB Assay	[PMID: 36170799]
T47D	IC₅₀	12780 nM Compound: AZD1775	Antiproliferative activity against human T47D cells incubated for 72 hrs by Celltiter-glo assay Antiproliferative activity against human T47D cells incubated for 72 hrs by Celltiter-glo assay	[PMID: 37167712]

In Vitro

Adavosertib (MK-1775) enhances the cytotoxic effects of 5-FU in p53-deficient human colon cancer cells. Adavosertib (MK-1775) inhibits CDC2 Y15 phosphorylation in cells, abrogates DNA damaged checkpoints induced by 5-FU treatment, and causes premature entry of mitosis determined by induction of Histone H3 phosphorylation^[1].
Adavosertib (MK-1775) abrogates the radiation-induced G2 block in p53-defective cells but not in p53 wild-type lines^[2].
The combination of NSC 613327 with Adavosertib (MK-1775) produces robust anti-tumor activity and remarkably enhances tumor regression response (4.01 fold) compared to NSC 613327 treatment in p53-deficient tumors^[3].

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

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (199.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9976 mL	9.9880 mL	19.9760 mL
5 mM	0.3995 mL	1.9976 mL	3.9952 mL
10 mM	0.1998 mL	0.9988 mL	1.9976 mL

View the Complete Stock Solution Preparation Table

* 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.

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

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 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (4.16 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 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 (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 0.5% Methylcellulose/saline water
Solubility: 5 mg/mL (9.99 mM); Suspended solution; Need ultrasonic

Pureté et documentation

Purity: 99.96%

Fiche technique (279 KB) SDS (393 KB)

COA (248 KB) LCMS (148 KB) Elemental Analysis Report (106 KB)

Instruction de manipulation (2659 KB)

Références

[1]. Hirai H, et al. MK-1775, a small molecule Wee1 inhibitor, enhances anti-tumor efficacy of various DNA-damaging agents, including 5-FU. Cancer Biol Ther. 2010 Apr;9(7):514-22. [Content Brief]

[2]. Bridges KA, et al. MK-1775, a novel Wee1 kinase inhibitor, radiosensitizes p53-defective human tumor cells. Clin Cancer Res. 2011 Sep 1;17(17):5638-48. Epub 2011 Jul 28. [Content Brief]

[3]. Rajeshkumar NV, et al. MK-1775, a potent Wee1 inhibitor, synergizes with NSC 613327 to achieve tumor regressions, selectively in p53-deficient pancreatic cancer xenografts.Clin Cancer Res. 2011 May 1;17(9):2799-806. Epub 2011 Mar 9. [Content Brief]

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