Art. -Nr.: HY-10971

Alisertib

(Synonyms: MLN 8237)

73 Cited Publications

Kundenbewertung

Based on 73 publication(s) in Google Scholar

Alisertib (MLN 8237) is an orally active and selective Aurora A kinase inhibitor (IC₅₀=1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib (MLN 8237) induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway in leukemic cells. Antitumor activity.

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Reinheit: 99.36%
CAS. Nr.: 1028486-01-2
Formel: C₂₇H₂₀ClFN₄O₄
Molecular Weight:518.92

Speicherung:

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

Alisertib Chemical Structure

CAS. Nr.: 1028486-01-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (73)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[3]

Aurora A

1.2 nM (IC₅₀)

Aurora B

396.5 nM (IC₅₀)

Alle Aurora Kinase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	95 nM Compound: 29, MLN-8237	Antiproliferative activity against human HCT116 cells after 72 hrs by WST8 assay Antiproliferative activity against human HCT116 cells after 72 hrs by WST8 assay	[PMID: 25625617]
HCT-116	GI₅₀	0.03 μM Compound: 10, alisertib	Cytotoxicity against human HCT116 cells assessed as inhibition of cell proliferation by BrdU incorporation assay Cytotoxicity against human HCT116 cells assessed as inhibition of cell proliferation by BrdU incorporation assay	[PMID: 26101564]
HCT-116	IC₅₀	1.5 μM Compound: 10, alisertib	Inhibition of aurora kinase B in human HCT116 cells assessed as inhibition of histone H3 phosphorylation by immunofluorescence analysis Inhibition of aurora kinase B in human HCT116 cells assessed as inhibition of histone H3 phosphorylation by immunofluorescence analysis	[PMID: 26101564]
HCT-116	IC₅₀	7 nM Compound: 10, alisertib	Inhibition of aurora kinase A autophosphorylation at T288 in human HCT116 cells by immunofluorescence analysis Inhibition of aurora kinase A autophosphorylation at T288 in human HCT116 cells by immunofluorescence analysis	[PMID: 26101564]
HCT-116	IC₅₀	32 μM Compound: MLN-8237	Antiproliferative activity against human HCT116 cells measured after 96 hrs by Brdu incorporation-based ELISA Antiproliferative activity against human HCT116 cells measured after 96 hrs by Brdu incorporation-based ELISA	[PMID: 31381325]
HCT-15	IC₅₀	740 nM Compound: 29, MLN-8237	Antiproliferative activity against human HCT15 cells after 72 hrs by WST8 assay Antiproliferative activity against human HCT15 cells after 72 hrs by WST8 assay	[PMID: 25625617]
HL-60	IC₅₀	74 nM Compound: 29, MLN-8237	Antiproliferative activity against human HL60 cells after 72 hrs by WST8 assay Antiproliferative activity against human HL60 cells after 72 hrs by WST8 assay	[PMID: 25625617]
HT-29	IC₅₀	330 nM Compound: 29, MLN-8237	Antiproliferative activity against human HT-29 cells after 72 hrs by WST8 assay Antiproliferative activity against human HT-29 cells after 72 hrs by WST8 assay	[PMID: 25625617]
LC-2-ad	IC₅₀	77 nM Compound: 29, MLN-8237	Antiproliferative activity against human LC2/ad cells after 72 hrs by WST8 assay Antiproliferative activity against human LC2/ad cells after 72 hrs by WST8 assay	[PMID: 25625617]
LU-99A	IC₅₀	62 nM Compound: 29, MLN-8237	Antiproliferative activity against human LU99A cells after 72 hrs by WST8 assay Antiproliferative activity against human LU99A cells after 72 hrs by WST8 assay	[PMID: 25625617]
MIA PaCa-2	IC₅₀	130 nM Compound: 29, MLN-8237	Antiproliferative activity against human MIAPaCa2 cells after 72 hrs by WST8 assay Antiproliferative activity against human MIAPaCa2 cells after 72 hrs by WST8 assay	[PMID: 25625617]
MKN-45	IC₅₀	93 nM Compound: 29, MLN-8237	Antiproliferative activity against human MKN45 cells after 72 hrs by WST8 assay Antiproliferative activity against human MKN45 cells after 72 hrs by WST8 assay	[PMID: 25625617]
MRC5	IC₅₀	>10000 nM Compound: 29, MLN-8237	Antiproliferative activity against human MRC5 cells after 72 hrs by WST8 assay Antiproliferative activity against human MRC5 cells after 72 hrs by WST8 assay	[PMID: 25625617]
MV4-11	IC₅₀	1.2 nM Compound: 17	Induction of cell cycle arrest in human MV4-11 cells assessed as accumulation of cells at G2/M phase measured after 12 hrs Induction of cell cycle arrest in human MV4-11 cells assessed as accumulation of cells at G2/M phase measured after 12 hrs	[PMID: 36306471]
NCI-H358	IC₅₀	100 nM Compound: 29, MLN-8237	Antiproliferative activity against human NCI-H358 cells after 72 hrs by WST8 assay Antiproliferative activity against human NCI-H358 cells after 72 hrs by WST8 assay	[PMID: 25625617]
PC-14	IC₅₀	170 nM Compound: 29, MLN-8237	Antiproliferative activity against human PC14 cells after 72 hrs by WST8 assay Antiproliferative activity against human PC14 cells after 72 hrs by WST8 assay	[PMID: 25625617]
Sf9	IC₅₀	1 nM Compound: 10, alisertib	Inhibition of recombinant mouse aurora kinase A expressed in insect Sf9 cells using biotin-GLRRASLG as substrate in presence of [gamma-33P]ATP Inhibition of recombinant mouse aurora kinase A expressed in insect Sf9 cells using biotin-GLRRASLG as substrate in presence of [gamma-33P]ATP	[PMID: 26101564]

In Vitro

Alisertib (MLN 8237) leads the MM cells to mitotic spindle abnormalities, mitotic accumulation, as well as inhibition of cell proliferation through apoptosis and senescence. Alisertib up-regulates p53 and tumor suppressor genes p21 and p27^[1].
The decreased activity of Alisertib (MLN 8237) for the T217D/W277E Aurora A/TPX2 complex may reflect the increased affinity for ATP induced by cofactor binding to Aurora A^[2].
Alisertib (MLN 8237) inhibits cell proliferation with IC₅₀s ranging from 15 to 469 nM in different tumer cell lines^[4].

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

In Vivo

Alisertib (MLN 8237) (30 mg/kg, p.o.) significantly reduces tumor burden and increases overall survival in xenograft-murine model of human-MM^[1].
Alisertib (3-30 mg/kg; p.o.; once daily for 3 weeks) causes tumor growth inhibition in solid tumor xenograft models^[4].

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

Animal Model:

Nude mice bearing HCT-116 colon tumor xenograft^[4]
Dosage:

3, 10, or 30 mg/kg
Administration:

P.o.; once daily for 3 weeks
Result:

Resulted in a dose-dependent TGI (tumor growth inhibition) of 43.3%, 84.2%, and 94.7% for the 3, 10, and 30 mg/kg groups,respectively.

Clinical Trial

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

Chemical Information

CAS. Nr. 1028486-01-2
Appearance Solid
Molecular Weight 518.92
Formel C₂₇H₂₀ClFN₄O₄
Color Off-white to yellow
SMILES

O=C(C1=CC=C(C=C1OC)NC2=NC=C3CN=C(C4=CC(Cl)=CC=C4C3=N2)C5=C(C=CC=C5F)OC)O
Synonyms

MLN 8237
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (73)

All IFIHCWB

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Journal Impact Factor

Cell

Dynamic Remodeling of Membrane Composition Drives Cell Cycle through Primary Cilia Excision. [Abstract]

2017 Jan 12;168(1-2):264-279.e15. PMID: 28086093
J Hepatol

FOSL1 promotes cholangiocarcinoma via transcriptional effectors that could be therapeutically targeted. [Abstract]

2021 Aug;75(2):363-376. PMID: 33887357
Adv Funct Mater

2024 Nov 04.
Cancer Res

HAND2 assists MYCN enhancer invasion to regulate a noradrenergic neuroblastoma phenotype. [Abstract]

2023 Mar 2;83(5):686-699. PMID: 36598365
Hepatology

Arid1a deficiency promotes hepatocyte hyperpolyploidy and drives intrahepatic cholangiocarcinoma in mice. [Abstract]

2025 Jun 9. PMID: 40489743
Nat Commun

Selective targeting of genome amplifications and repeat elements by CRISPR-Cas9 nickases to promote cancer cell death. [Abstract]

2025 Jun 2;16(1):5126. PMID: 40456709
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
J Clin Invest

Targeting Wnt/β-Catenin and circadian regulator restores PRC2/EZH2 controlled chromatin bivalency and suppresses cell state diversity. [Abstract]

2026 Mar 17:e200260. PMID: 41842971
Leukemia

Unraveling the impact of crizotinib to promote megakaryopoiesis for alleviating thrombocytopenia in myelodysplastic neoplasms. [Abstract]

2025 Aug 14. PMID: 40813622
Theranostics

Genomic analysis of liver cancer unveils novel driver genes and distinct prognostic features. [Abstract]

2018 Feb 12;8(6):1740-1751. PMID: 29556353
Protein Cell

Glutamine signaling specifically activates c-Myc and Mcl-1 to Facilitate cancer cell proliferation and survival. [Abstract]

2025 May 4:pwaf029. PMID: 40338031
J Exp Clin Cancer Res

Repurposed AT9283 triggers anti-tumoral effects by targeting MKK3 oncogenic functions in Colorectal Cancer. [Abstract]

2024 Aug 20;43(1):234. PMID: 39164711
J Nanobiotechnology

Targeting AURKA with multifunctional nanoparticles in CRPC therapy. [Abstract]

2024 Dec 30;22(1):803. PMID: 39734237
MedComm (2020)

Integrated Multi-Omics Profiling to Characterize Molecular Subtypes and Reveal Potential Therapeutic Strategies for Colorectal Cancer. [Abstract]

2025 Dec 8;6(12):e70492. PMID: 41377767
Cell Rep Med

Modeling high-risk Wilms tumors enables the discovery of therapeutic vulnerability. [Abstract]

2024 Sep 27:101770. PMID: 39368485
Clin Cancer Res

Unexpected Activities in Regulating Ciliation Contribute to Off-target Effects of Targeted Drugs. [Abstract]

2019 Jul 1;25(13):4179-4193. PMID: 30867219
Cancer Lett

Aurora kinase A inhibition as a synthetic lethality strategy in ARID1A-mutated gastroenteropancreatic neuroendocrine carcinoma. [Abstract]

2025 Sep 16:634:218033. PMID: 40962046
Cell Death Dis

Aurora-A/FOXO3A/SKP2 axis promotes tumor progression in clear cell renal cell carcinoma and dual-targeting Aurora-A/SKP2 shows synthetic lethality. [Abstract]

2022 Jul 13;13(7):606. PMID: 35831273
EMBO J

CEP192 localises mitotic Aurora-A activity by priming its interaction with TPX2. [Abstract]

2024 Nov;43(22):5381-5420. PMID: 39327527
NPJ Precis Oncol

Targeting high-risk MYC-overexpressed osteosarcoma with an Aurora kinase inhibitor:--results from a pilot umbrella trial. [Abstract]

2025 Dec 10. PMID: 41372533
Neoplasia

Combining selinexor with alisertib to target the p53 pathway in neuroblastoma. [Abstract]

2022 Apr:26:100776. PMID: 35217309
Neoplasia

The synergy of BET inhibitors with aurora A kinase inhibitors in MYCN-amplified neuroblastoma is heightened with functional TP53. [Abstract]

2021 Jun;23(6):624-633. PMID: 34107377
J Transl Med

Doxorubicin synergizes bortezomib-induced multiple myeloma cell death by inhibiting aggresome formation and augmenting endoplasmic reticulum/Golgi stress and apoptosis. [Abstract]

2024 Dec 3;22(1):1095. PMID: 39623468
Oncogene

RB loss determines selective resistance and novel vulnerabilities in ER-positive breast cancer models. [Abstract]

2022 Jul;41(27):3524-3538. PMID: 35676324
Cell Death Discov

RB loss sensitizes triple-negative breast cancer to apoptosis induced by cellular stress. [Abstract]

2025 Nov 24;11(1):543. PMID: 41285729
Cell Rep

PLK1 blockade enhances the anti-tumor effect of MAPK inhibition in pancreatic ductal adenocarcinoma. [Abstract]

2025 Apr 5;44(4):115541. PMID: 40188436
Br J Cancer

Inhibition of the AURKA/YAP1 axis is a promising therapeutic option for overcoming cetuximab resistance in colorectal cancer stem cells. [Abstract]

2024 May;130(8):1402-1413. PMID: 38467828
EMBO Rep

The GCN2/eIF2αK stress kinase regulates PP1 to ensure mitotic fidelity. [Abstract]

2023 Aug 3;24(8):e56100. PMID: 37291955
EMBO Rep

HDAC2 promotes loss of primary cilia in pancreatic ductal adenocarcinoma. [Abstract]

2017 Feb;18(2):334-343. PMID: 28028031
Cancer Cell Int

Silencing of AURKA augments the antitumor efficacy of the AURKA inhibitor MLN8237 on neuroblastoma cells. [Abstract]

2020 Jan 7;20:9. PMID: 31920463
J Invest Dermatol

Actionable genetic screens unveil targeting of AURKA, MEK and fatty acid metabolism as an alternative therapeutic approach for advanced melanoma. [Abstract]

2023 Oct;143(10):1993-2006.e10. PMID: 37003468
Biochem Pharmacol

Palmatine induces G2/M phase arrest and mitochondrial-associated pathway apoptosis in colon cancer cells by targeting AURKA. [Abstract]

2020 May;175:113933. PMID: 32224138
Cells

Suppressing PD-L1 Expression via AURKA Kinase Inhibition Enhances Natural Killer Cell-Mediated Cytotoxicity against Glioblastoma. [Abstract]

2024 Jul 6;13(13):1155. PMID: 38995006
Commun Biol

PIP2 determines length and stability of primary cilia by balancing membrane turnovers. [Abstract]

2022 Jan 25;5(1):93. PMID: 35079141
Int J Mol Sci

Aurora Kinase A and Bcl-xL Inhibition Suppresses Metastasis in Triple-Negative Breast Cancer. [Abstract]

2022 Sep 2;23(17):10053. PMID: 36077449
Int J Mol Sci

Aurora Kinase A Is Involved in Controlling the Localization of Aquaporin-2 in Renal Principal Cells. [Abstract]

2022 Jan 11;23(2):763. PMID: 35054947
Int J Mol Sci

Evaluation of Protein Kinase Inhibitors with PLK4 Cross-Over Potential in a Pre-Clinical Model of Cancer. [Abstract]

2019 Apr 29;20(9):2112. PMID: 31035676
Cell Oncol (Dordr)

Novel preclinical gastroenteropancreatic neuroendocrine neoplasia models demonstrate the feasibility of mutation-based targeted therapy. [Abstract]

2022 Dec;45(6):1401-1419. PMID: 36269546
Eur J Pharmacol

Doxorubicin-mediated retardation of aggresome formation enhances Carfilzomib-induced cell death synergistically by augmenting ER stress and proapoptotic signaling. [Abstract]

2025 Dec 5:1008:178303. PMID: 41183585
Cell Rep Methods

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

2023 Oct 23;3(10):100599. PMID: 37797618
Cancer Sci

TP-0903 Suppresses Aurora A-PLK1 Signaling to Inhibit Proliferation of a Myelodysplastic Syndrome-Derived Cell Line. [Abstract]

2025 Jul 28. PMID: 40722126
ACS Omega

Preclinical Evaluation of JAB-2485, a Potent AURKA Inhibitor with High Selectivity and Favorable Pharmacokinetic Properties. [Abstract]

2024 May 3;9(19):21416-21425. PMID: 38764682
J Cell Mol Med

Inactivation of CDK12 Enhances Mitochondrial Efficiency to Suppress DNA Damage. [Abstract]

2026 Apr;30(7):e71101. PMID: 41896195
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
FASEB J

Ganetespib limits ciliation and cystogenesis in autosomal-dominant polycystic kidney disease (ADPKD). [Abstract]

2018 May;32(5):2735-2746. PMID: 29401581

Alisertib purchased from MedChemExpress. Usage Cited in: FASEB J. 2018 May;32(5):2735-2746. [Abstract]

Representative immunofluorescence (IF) image and graph with frequency of ciliated WT or Pkd12/2 murine renal epithelial cells at 2 h after treatment with vehicle (V), Ganetespib (G), or Alisertib (A) to inhibit AURKA, or (C) combination of Alisertib and Ganetespib. On IF, acetylated a-tubulin (red); g-tubulin (green); DAPI (blue).
iScience

Combination therapy with alisertib enhances the anti-tumor immunity induced by a liver cancer vaccine. [Abstract]

2025 Mar 15;28(4):112120. PMID: 40230537
J Biol Chem

Targeting the mitotic kinase NEK2 enhances CDK4/6 inhibitor efficacy by potentiating genome instability. [Abstract]

2025 Jan 16:108196. PMID: 39826695
Exp Cell Res

The aberrantly activated AURKB supports and complements the function of AURKA in CALR mutated cells through regulating the cell growth and differentiation. [Abstract]

2025 Jan 15;444(2):114377. PMID: 39706286
Toxicol Appl Pharmacol

Alisertib shows negligible potential for perpetrating pharmacokinetic drug-drug interactions on ABCB1, ABCG2 and cytochromes P450, but acts as dual-activity resistance modulator through the inhibition of ABCC1 transporter. [Abstract]

2022 Jan 1:434:115823. PMID: 34896433
Breast Cancer Res Treat

Combined inhibition of Aurora A and p21-activated kinase 1 as a new treatment strategy in breast cancer. [Abstract]

2019 Sep;177(2):369-382. PMID: 31254157
Am J Cancer Res

Epigenetic heterogeneity promotes acquired resistance to BET bromodomain inhibition in ovarian cancer. [Abstract]

2021 Jun 15;11(6):3021-3038. PMID: 34249442
Immun Inflamm Dis

Adiponectin Inhibits AURKA to Suppress Inflammation in TNF-α-induced Keratinocytes and Attenuates Psoriatic Dermatitis in Mice. [Abstract]

2026 Mar;14(3):e70407. PMID: 41873121
PLoS One

A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]

2024 Nov 1;19(11):e0308647. PMID: 39485774
PLoS One

Chorioallantoic membrane (CAM) assay to study treatment effects in diffuse intrinsic pontine glioma. [Abstract]

2022 Feb 14;17(2):e0263822. PMID: 35157705
Biochem Biophys Res Commun

ZNF468 inhibits irradiation-induced G2/M cell cycle arrest and apoptosis by facilitating AURKA transcription in Esophageal Squamous Cell Carcinoma. [Abstract]

2024 Apr 9:703:149687. PMID: 38368674
Clin Med Insights Oncol

Exploring the Clinical Implications of RPL3 Presence in BRCA-Associated Cancers: Unraveling the Interplay With Cancer Immunity. [Abstract]

2024 Oct 16:18:11795549241285387. PMID: 39429685
bioRxiv

Ferrous Iron Accumulation Is a Hallmark and Therapeutic Vulnerability of Therapy-Induced Senescence. [Abstract]

2026 May 23:2026.05.20.726695. PMID: 42239384
bioRxiv

Radiation synergizes with BET inhibition to stimulate durable, systemic anti-tumor immunity in murine cancer models. [Abstract]

2026 Feb 18:2026.02.16.706212. PMID: 41757027
bioRxiv

2025 Nov 24.
bioRxiv

2025 Sep 15.
bioRxiv

Bacterial ubiquitin ligase engineered for small molecule and protein target identification. [Abstract]

2025 Mar 22:2025.03.20.644192. PMID: 40166235
bioRxiv

2024 October 01.
Res Sq

2024 Oct 14.
bioRxiv

PAIRWISE: Deep Learning-based Prediction of Effective Personalized Drug Combinations in Cancer. [Abstract]

2024 Nov 6:2024.11.04.621884. PMID: 39574568
bioRxiv

2023 Aug 12.
bioRxiv

2023 Aug 13.
Research Square Preprint

2023 Apr 25.
bioRxiv

2021 Feb 5.
Patent

US20180263995A1.
Technical University of Munich

24.01.2018.
Oncotarget

Molecular-genetic profiling and high-throughput in vitro drug screening in NUT midline carcinoma-an aggressive and fatal disease. [Abstract]

2017 Dec 2;8(68):112313-112329. PMID: 29348827
Johns Hopkins University

2017 Mar.
Drexel University

2016 Nov.

Alisertib purchased from MedChemExpress. Usage Cited in: Drexel University. 2016 Nov.

Alisertib and combination treatment suppress proliferation in BT474 orthotopic tumors as shown by decrease in Ki-67, which is statistically significantly different between vehicle and combination treatment, FRAX1036 and Alisertib, and FRAX1036 and combination treatment.

Alisertib purchased from MedChemExpress. Usage Cited in: Drexel University. 2016 Nov.

Alisertib enhances FRAX1036 inhibitory effect on PAK1 phosphorylation in BT474 xenograft model.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 25 mg/mL (48.18 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

1.9271 mL

9.6354 mL

19.2708 mL

5 mM

0.3854 mL

1.9271 mL

3.8542 mL

10 mM

0.1927 mL

0.9635 mL

1.9271 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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: 2.08 mg/mL (4.01 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 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% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.01 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

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: 50% PEG300 50% Saline

Solubility: 10 mg/mL (19.27 mM); Suspended solution; Need ultrasonic

Protocol 2

Add each solvent one by one: 0.5% CMC-Na/saline water

Solubility: 5 mg/mL (9.64 mM); Suspended solution; Need ultrasonic

Protocol 3

Add each solvent one by one: 15% Cremophor EL 85% Saline

Solubility: 10 mg/mL (19.27 mM); Suspended solution; Need ultrasonic

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
SDS (393 KB)
- English - EN (393 KB)
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- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
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- Portuguese - PT (393 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)
Handling Instructions (2659 KB)

Verweise

[1]. Güllü G, et al. A novel Aurora-A kinase inhibitor MLN8237 induces cytotoxicity and cell-cycle arrest in multiple myeloma Blood June 24, 2010 vol. 115 no. 25 5202-5213. [Content Brief]

[2]. Sloane DA, et al. Drug-Resistant Aurora A Mutants for Cellular Target Validation of the Small Molecule Kinase Inhibitors MLN8054 and MLN8237 ACS Chem. Biol., 2010, 5 (6), pp 563-576. [Content Brief]

[3]. Bavetsias V, et al. Aurora Kinase Inhibitors: Current Status and Outlook. Front Oncol. 2015 Dec 21;5:278. [Content Brief]

[4]. Manfredi MG, et al. Characterization of Alisertib (MLN8237), an investigational small-molecule inhibitor of aurora A kinase using novel in vivo pharmacodynamic assays.Clin Cancer Res. 2011 Dec 15;17(24):7614-7624. [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
DMSO	1 mM	1.9271 mL	9.6354 mL	19.2708 mL	48.1770 mL
	5 mM	0.3854 mL	1.9271 mL	3.8542 mL	9.6354 mL
	10 mM	0.1927 mL	0.9635 mL	1.9271 mL	4.8177 mL
	15 mM	0.1285 mL	0.6424 mL	1.2847 mL	3.2118 mL
	20 mM	0.0964 mL	0.4818 mL	0.9635 mL	2.4088 mL
	25 mM	0.0771 mL	0.3854 mL	0.7708 mL	1.9271 mL
	30 mM	0.0642 mL	0.3212 mL	0.6424 mL	1.6059 mL
	40 mM	0.0482 mL	0.2409 mL	0.4818 mL	1.2044 mL

Keywords

Alisertib

73 Cited Publications

100 mg Angebot einholen

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Alisertib

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Clinical Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Rare Diseases Drug Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

Epigenetics Compound Library Mini

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

RNA Binding Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Alisertib

Alle Aurora Kinase Isoform-spezifische Produkte anzeigen

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Chemical Information

Publications (73)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

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Complete Stock Solution Preparation Table

Alisertib Related Classifications

Art. -Nr.: HY-10971