Alisertib
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.36%
- No. CAS: 1028486-01-2
- Fòrmula: C27H20ClFN4O4
- Peso molecular:518.92
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Alisertib
More- Cell. 2017 Jan 12;168(1-2):264-279.e15. [Abstract]
- J Hepatol. 2021 Aug;75(2):363-376. [Abstract]
- Adv Funct Mater. 2024 Nov 04.
- Cancer Res. 2023 Mar 2;83(5):686-699. [Abstract]
- Hepatology. 2025 Jun 9. [Abstract]
- Nat Commun. 2025 Jun 2;16(1):5126. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- J Clin Invest. 2026 Mar 17:e200260. [Abstract]
- Leukemia. 2025 Aug 14. [Abstract]
- Theranostics. 2018 Feb 12;8(6):1740-1751. [Abstract]
- Protein Cell. 2025 May 4:pwaf029. [Abstract]
- J Exp Clin Cancer Res. 2024 Aug 20;43(1):234. [Abstract]
- J Nanobiotechnology. 2024 Dec 30;22(1):803. [Abstract]
- MedComm (2020). 2025 Dec 8;6(12):e70492. [Abstract]
- Cell Rep Med. 2024 Sep 27:101770. [Abstract]
- Clin Cancer Res. 2019 Jul 1;25(13):4179-4193. [Abstract]
- Cancer Lett. 2025 Sep 16:634:218033. [Abstract]
- Cell Death Dis. 2022 Jul 13;13(7):606. [Abstract]
- EMBO J. 2024 Nov;43(22):5381-5420. [Abstract]
- NPJ Precis Oncol. 2025 Dec 10. [Abstract]
- Neoplasia. 2022 Apr:26:100776. [Abstract]
- Neoplasia. 2021 Jun;23(6):624-633. [Abstract]
- J Transl Med. 2024 Dec 3;22(1):1095. [Abstract]
- Oncogene. 2022 Jul;41(27):3524-3538. [Abstract]
- Cell Death Discov. 2025 Nov 24;11(1):543. [Abstract]
- Cell Rep. 2025 Apr 5;44(4):115541. [Abstract]
- Br J Cancer. 2024 May;130(8):1402-1413. [Abstract]
- EMBO Rep. 2023 Aug 3;24(8):e56100. [Abstract]
- EMBO Rep. 2017 Feb;18(2):334-343. [Abstract]
- Cancer Cell Int. 2020 Jan 7;20:9. [Abstract]
- J Invest Dermatol. 2023 Oct;143(10):1993-2006.e10. [Abstract]
- Biochem Pharmacol. 2020 May;175:113933. [Abstract]
- Cells. 2024 Jul 6;13(13):1155. [Abstract]
- Commun Biol. 2022 Jan 25;5(1):93. [Abstract]
- Int J Mol Sci. 2022 Sep 2;23(17):10053. [Abstract]
- Int J Mol Sci. 2022 Jan 11;23(2):763. [Abstract]
- Int J Mol Sci. 2019 Apr 29;20(9):2112. [Abstract]
- Cell Oncol (Dordr). 2022 Dec;45(6):1401-1419. [Abstract]
- Eur J Pharmacol. 2025 Dec 5:1008:178303. [Abstract]
- Cell Rep Methods. 2023 Oct 23;3(10):100599. [Abstract]
- Cancer Sci. 2025 Jul 28. [Abstract]
- ACS Omega. 2024 May 3;9(19):21416-21425. [Abstract]
- J Cell Mol Med. 2026 Apr;30(7):e71101. [Abstract]
- Biochim Biophys Acta Mol Basis Dis. 2024 Feb 10;1870(4):167062. [Abstract]
- FASEB J. 2018 May;32(5):2735-2746. [Abstract]
- iScience. 2025 Mar 15;28(4):112120. [Abstract]
- J Biol Chem. 2025 Jan 16:108196. [Abstract]
- Exp Cell Res. 2025 Jan 15;444(2):114377. [Abstract]
- Toxicol Appl Pharmacol. 2022 Jan 1:434:115823. [Abstract]
- Breast Cancer Res Treat. 2019 Sep;177(2):369-382. [Abstract]
- Am J Cancer Res. 2021 Jun 15;11(6):3021-3038. [Abstract]
- Immun Inflamm Dis. 2026 Mar;14(3):e70407. [Abstract]
- PLoS One. 2024 Nov 1;19(11):e0308647. [Abstract]
- PLoS One. 2022 Feb 14;17(2):e0263822. [Abstract]
- Biochem Biophys Res Commun. 2024 Apr 9:703:149687. [Abstract]
- Clin Med Insights Oncol. 2024 Oct 16:18:11795549241285387. [Abstract]
- bioRxiv. 2026 May 23:2026.05.20.726695. [Abstract]
- bioRxiv. 2026 Feb 18:2026.02.16.706212. [Abstract]
- bioRxiv. 2025 Nov 24.
- bioRxiv. 2025 Sep 15.
- bioRxiv. 2025 Mar 22:2025.03.20.644192. [Abstract]
- bioRxiv. 2024 October 01.
- Res Sq. 2024 Oct 14.
- bioRxiv. 2024 Nov 6:2024.11.04.621884. [Abstract]
- 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. 2017 Dec 2;8(68):112313-112329. [Abstract]
- Johns Hopkins University. 2017 Mar.
- Drexel University. 2016 Nov.
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Ver todos los productos específicos de isoformas Aurora Kinase
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Actividad biológica
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Aurora A 1.2 nM (IC50) |
Aurora B 396.5 nM (IC50) |
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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
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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
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[PMID: 26101564] |
| HCT-116 | IC50 |
1.5 μM
Compound: 10, alisertib
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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
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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
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[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
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[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] |
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.
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.
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Animal Model:Nude mice bearing HCT-116 colon tumor xenograft[4]
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Dosage:3, 10, or 30 mg/kg
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Administration:P.o.; once daily for 3 weeks
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1028486-01-2
-
Appearance Solid
-
Peso molecular 518.92
-
Fòrmula C27H20ClFN4O4
-
Color Off-white to yellow
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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
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Synonyms
MLN 8237
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (73)
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Journal Impact Factor
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Most Recent
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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 -
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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
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
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
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
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
2023 Aug 3;24(8):e56100. PMID: 37291955 -
EMBO Rep
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
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
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).
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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 -
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bioRxiv
Bacterial ubiquitin ligase engineered for small molecule and protein target identification. [Abstract]2025 Mar 22:2025.03.20.644192. PMID: 40166235 -
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bioRxiv
PAIRWISE: Deep Learning-based Prediction of Effective Personalized Drug Combinations in Cancer. [Abstract]2024 Nov 6:2024.11.04.621884. PMID: 39574568 -
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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 -
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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.
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline 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.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 10 mg/mL (19.27 mM); Suspended solution; Need ultrasonic
Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 5 mg/mL (9.64 mM); Suspended solution; Need ultrasonic
Add each solvent one by one: 15% Cremophor EL 85% Saline
Solubility: 10 mg/mL (19.27 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (284 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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]
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.
| 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 |
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