TAK-901 hydrochloride
Based on 5 publication(s) in Google Scholar
TAK-901 hydrochloride is a multi-targeted aurora inhibitor with IC50s of 21 and 15 nM for aurora A and B, respectively.
For research use only. We do not sell to patients.
- CAS No.: 934542-50-4
- Formula: C28H33ClN4O3S
- Molecular Weight:541.10
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) TAK-901 hydrochloride
MoreAll Aurora Kinase Isoforms
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Biological Activity
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Aurora B 15 nM (IC50) |
Aurora A 21 nM (IC50) |
TAK-901 exhibits time-dependent, tight-binding inhibition of Aurora B, but not Aurora A[1].
TAK-901 suppresses histone H3 phosphorylation in a dose-dependent manner with an EC50
value of 0.16 μM in PC3 cells[1].
TAK-901 is a substrate of the P-glycoprotein (PgP) drug efflux pump, as shown by the decrease in
EC50 from 38 nM in the uterine sarcoma MES-SA cells to more than 50 μM in drug-resistant MES-SA/Dx5 expressing high levels of PgP[1].
| Cell line | EC50 (μM) |
|---|---|
| A2780 | 0.085 |
| A375 | 0.39 |
| A498 | 0.2 |
| A549 | 0.13 |
| COLO205 | 0.11 |
| DLD1 | 1.5 |
| H226 | 0.11 |
| H358 | 0.077 |
| H460 | 0.81 |
| HT29 | 0.062 |
| MDA-MB-435S | 0.12 |
| MES-SA | 0.043 |
| MKN-45 | 0.16 |
| PC3 | 0.19 |
| IMR-90 | 0.088 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 934542-50-4
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Molecular Weight 541.10
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Formula C28H33ClN4O3S
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SMILES
O=C(NC1CCN(CC1)C)C2=C(C3=C(C4=CC(C)=CN=C4N3)C(C5=CC=CC(S(=O)(CC)=O)=C5)=C2)C.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (5)
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Journal Impact Factor
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Most Recent
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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 -
EBioMedicine
A chemical genetic screen identifies Aurora kinases as a therapeutic target in EGFR T790M negative, gefitinib-resistant head and neck squamous cell carcinoma (HNSCC). [Abstract]2021 Feb:64:103220. PMID: 33529999 -
Sci Data
High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]2024 Sep 19;11(1):1024. PMID: 39300112 -
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Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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