Alisertib sodium
Based on 75 publication(s) in Google Scholar
Alisertib (MLN 8237) sodium 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 sodium induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway in leukemic cells. Antitumor activity.
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- CAS No.: 1028486-06-7
- Formule: C27H19ClFN4NaO4
- Masse moléculaire:540.91
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
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Publications Citing Use of MedChemExpress (MCE) Alisertib sodium
More- Cell. 2017 Jan 12;168(1-2):264-279.e15. [Abstract]
- J Hepatol. 2021 Aug;75(2):363-376. [Abstract]
- Cancer Res. 2023 Mar 2;83(5):686-699. [Abstract]
- Adv Funct Mater. 2024 Nov 04.
- Protein Cell. 2025 Nov 1;16(11):968-984. [Abstract]
- Nat Commun. 2025 Jun 2;16(1):5126. [Abstract]
- Hepatology. 2025 Jun 9. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- J Nanobiotechnology. 2024 Dec 30;22(1):803. [Abstract]
- Theranostics. 2018 Feb 12;8(6):1740-1751. [Abstract]
- J Clin Invest. 2026 Mar 17:e200260. [Abstract]
- J Exp Clin Cancer Res. 2024 Aug 20;43(1):234. [Abstract]
- MedComm (2020). 2025 Dec 8;6(12):e70492. [Abstract]
- Cell Rep Med. 2024 Oct 15;5(10):101770. [Abstract]
- Cell Death Dis. 2022 Jul 13;13(7):606. [Abstract]
- Cancer Lett. 2025 Dec 1:634:218033. [Abstract]
- Phytomedicine. 2026 Apr 27. [Abstract]
- Clin Cancer Res. 2019 Jul 1;25(13):4179-4193. [Abstract]
- Cell Death Discov. 2025 Nov 24;11(1):543. [Abstract]
- NPJ Precis Oncol. 2025 Dec 10. [Abstract]
- J Transl Med. 2024 Dec 3;22(1):1095. [Abstract]
- Oncogene. 2022 Jul;41(27):3524-3538. [Abstract]
- Leukemia. 2025 Aug 14. [Abstract]
- EMBO J. 2024 Nov;43(22):5381-5420. [Abstract]
- Br J Cancer. 2024 May;130(8):1402-1413. [Abstract]
- Cell Rep. 2025 Apr 5;44(4):115541. [Abstract]
- J Invest Dermatol. 2023 Oct;143(10):1993-2006.e10. [Abstract]
- Cancer Cell Int. 2020 Jan 7:20:9. [Abstract]
- Biochem Pharmacol. 2020 May:175:113933. [Abstract]
- Cells. 2024 Jul 6;13(13):1155. [Abstract]
- EMBO Rep. 2023 Aug 3;24(8):e56100. [Abstract]
- EMBO Rep. 2017 Feb;18(2):334-343. [Abstract]
- Cell Rep Methods. 2023 Oct 23;3(10):100599. [Abstract]
- Commun Biol. 2022 Jan 25;5(1):93. [Abstract]
- Eur J Pharmacol. 2025 Dec 5:1008:178303. [Abstract]
- Cell Oncol (Dordr). 2022 Dec;45(6):1401-1419. [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]
- ACS Omega. 2024 May 3;9(19):21416-21425. [Abstract]
- Biochim Biophys Acta Mol Basis Dis. 2024 Feb 10;1870(4):167062. [Abstract]
- Cancer Sci. 2025 Jul 28. [Abstract]
- Neoplasia. 2022 Apr:26:100776. [Abstract]
- Neoplasia. 2021 Jun;23(6):624-633. [Abstract]
- J Cell Mol Med. 2026 Apr;30(7):e71101. [Abstract]
- iScience. 2025 Mar 15;28(4):112120. [Abstract]
- FASEB J. 2018 May;32(5):2735-2746. [Abstract]
- J Biol Chem. 2025 Feb;301(2):108196. [Abstract]
- Toxicol Appl Pharmacol. 2022 Jan 1:434:115823. [Abstract]
- Immun Inflamm Dis. 2026 Mar;14(3):e70407. [Abstract]
- Exp Cell Res. 2025 Jan 15;444(2):114377. [Abstract]
- Breast Cancer Res Treat. 2019 Sep;177(2):369-382. [Abstract]
- Am J Cancer Res. 2021 Jun 15;11(6):3021-3038. [Abstract]
- PLoS One. 2024 Nov 1;19(11):e0308647. [Abstract]
- PLoS One. 2022 Feb 14;17(2):e0263822. [Abstract]
- Clin Med Insights Oncol. 2024 Oct 16:18:11795549241285387. [Abstract]
- Clin Exp Pharmacol Physiol. 2026 Jun;53(6):e70132. [Abstract]
- Biochem Biophys Res Commun. 2024 Apr 9:703:149687. [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]
- Res Sq. 2024 Oct 14.
- bioRxiv. 2024 October 01.
- bioRxiv. 2024 Nov 6:2024.11.04.621884. [Abstract]
- bioRxiv. 2023 Aug 13.
- bioRxiv. 2023 Aug 12.
- 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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Voir tous les produits spécifiques à Isoform Aurora Kinase
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Activité biologique
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Aurora A 12.5 nM (IC50) |
Aurora B 396.5 nM (IC50) |
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.
Chemical Information
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CAS No. 1028486-06-7
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Masse moléculaire 540.91
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Formule C27H19ClFN4NaO4
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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[Na]
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Synonyms
MLN 8237 sodium
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (75)
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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 -
Cancer Res
HAND2 assists MYCN enhancer invasion to regulate a noradrenergic neuroblastoma phenotype. [Abstract]2023 Mar 2;83(5):686-699. PMID: 36598365 -
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Protein Cell
Glutamine signaling specifically activates c-Myc and Mcl-1 to Facilitate cancer cell proliferation and survival. [Abstract]2025 Nov 1;16(11):968-984. PMID: 40338031 -
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 -
Hepatology
Arid1a deficiency promotes hepatocyte hyperpolyploidy and drives intrahepatic cholangiocarcinoma in mice. [Abstract]2025 Jun 9. PMID: 40489743 -
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 Nanobiotechnology
2024 Dec 30;22(1):803. PMID: 39734237 -
Theranostics
Genomic analysis of liver cancer unveils novel driver genes and distinct prognostic features. [Abstract]2018 Feb 12;8(6):1740-1751. PMID: 29556353 -
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 -
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 -
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 Oct 15;5(10):101770. PMID: 39368485 -
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 -
Cancer Lett
Aurora kinase A inhibition as a synthetic lethality strategy in ARID1A-mutated gastroenteropancreatic neuroendocrine carcinoma. [Abstract]2025 Dec 1:634:218033. PMID: 40962046 -
Phytomedicine
Tongguanteng injection induces cell cycle arrest and drives ferroptosis through AURKA/KEAP1/NRF2 axis in breast cancer. [Abstract]2026 Apr 27. PMID: 42105703 -
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 -
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 -
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 -
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 -
Leukemia
Unraveling the impact of crizotinib to promote megakaryopoiesis for alleviating thrombocytopenia in myelodysplastic neoplasms. [Abstract]2025 Aug 14. PMID: 40813622 -
EMBO J
2024 Nov;43(22):5381-5420. PMID: 39327527 -
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 -
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 -
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 -
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 -
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 -
EMBO Rep
2023 Aug 3;24(8):e56100. PMID: 37291955 -
EMBO Rep
2017 Feb;18(2):334-343. PMID: 28028031 -
Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618 -
Commun Biol
2022 Jan 25;5(1):93. PMID: 35079141 -
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 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 -
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 -
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 -
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 -
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 -
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 Cell Mol Med
2026 Apr;30(7):e71101. PMID: 41896195 -
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 -
FASEB J
Ganetespib limits ciliation and cystogenesis in autosomal-dominant polycystic kidney disease (ADPKD). [Abstract]2018 May;32(5):2735-2746. PMID: 29401581
Alisertib sodium 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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J Biol Chem
Targeting the mitotic kinase NEK2 enhances CDK4/6 inhibitor efficacy by potentiating genome instability. [Abstract]2025 Feb;301(2):108196. PMID: 39826695 -
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 -
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 -
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 -
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 -
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 -
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 -
Clin Exp Pharmacol Physiol
Aurora A-Mediated Exosomal Secretion of miR-644a Promotes T-Lymphocyte Apoptosis Through the NOXA/p4E-BP1/MCL-1 Pathway. [Abstract]2026 Jun;53(6):e70132. PMID: 42203488 -
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 -
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 sodium 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 sodium purchased from MedChemExpress. Usage Cited in: Drexel University. 2016 Nov.
Alisertib enhances FRAX1036 inhibitory effect on PAK1 phosphorylation in BT474 xenograft model.
Pureté et documentation
Références
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Alisertib sodium Related Classifications
HY-10971A Related Classifications
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