1. Cell Cycle/DNA Damage Epigenetics
  2. Aurora Kinase
  3. TAK-901 hydrochloride

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.

TAK-901 hydrochloride Chemical Structure

TAK-901 hydrochloride Chemical Structure

CAS No. : 934542-50-4

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Description

TAK-901 hydrochloride is a multi-targeted aurora inhibitor with IC50s of 21 and 15 nM for aurora A and B, respectively[1].

IC50 & Target[1]

Aurora B

15 nM (IC50)

Aurora A

21 nM (IC50)

In Vitro

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.

In Vivo

TAK-901 (In A2780 and AML MV4-11 nude mice xenograft model) causes tumor stasis for 30 days at 30 and 40 mg/kg/injection, respectively[1].

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

Molecular Weight

541.10

Formula

C28H33ClN4O3S

CAS No.
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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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
TAK-901 hydrochloride
Cat. No.:
HY-12201A
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