Name: TAK-901
Brand: Selleck Chemicals
SKU: S2718
Availability: InStock
Rating: 5 (11 reviews)

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Quality Control

Batch: Purity: 99.83%

99.83

Related Targets	CDK HSP PD-1/PD-L1 ROCK Wee1 DNA/RNA Synthesis Microtubule Associated Ras KRas Casein Kinase
Other Aurora Kinase Inhibitors	Hesperadin Barasertib-HQPA (AZD2811) Alisertib (MLN8237) Tozasertib (VX-680) ZM 447439 MLN8054 Danusertib (PHA-739358) MK-5108 TCS7010 (Aurora A Inhibitor I) AMG-900

Solubility

In vitro
Batch:

DMSO : 101 mg/mL (200.14 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

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% ddH₂O

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	504.64	Formula	C₂₈H₃₂N₄O₃S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	934541-31-8	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CCS(=O)(=O)C1=CC=CC(=C1)C2=CC(=C(C3=C2C4=C(N3)N=CC(=C4)C)C)C(=O)NC5CCN(CC5)C

Mechanism of Action

Targets/IC₅₀/Ki	JAK3 1.2 nM c-Src 1.3 nM CLK2 <2.0 nM FGR <2.0 nM YES1 <2.0 nM LRRK2 3.0 nM FLT3 5.0 nM Fyn 5.3 nM ARG 5.6 nM Axl 5.8 nM Hck 5.8 nM SNF1LK2 6.0 nM Abl 6.4 nM RET 6.5 nM TrkA 6.7 nM LCK 6.8 nM PTK5 7.1 nM Fms 7.2 nM FGFR2 7.3 nM EphB1 8.9 nM Abl (T315I) 9.0 nM EphA1 9.1 nM ARK5 9.1 nM ITK 12 nM ALK2 13 nM CDK7 14 nM BLK 14 nM Aurora B-INCENP 15 nM JAK2 17 nM EphB2 18 nM Aurora A-TPX2 21 nM STK16 24 nM EphA2 24 nM BRK 25 nM EphB4 27 nM TNK2 27 nM FGFR1 28 nM EphA4 31 nM STK33 35 nM CLK1 45 nM AMPK 46 nM FES 48 nM SLK 49 nM Chk2 50 nM TYK2 54 nM BTK 55 nM FAK2 55 nM c-Kit 58 nM VEGFR2 60 nM FGFR3 65 nM ALK5 78 nM MAP3K9 80 nM CLK3 88 nM JAK1 93 nM
In vitro	TAK-901 inhibits Aurora A-TPX2 and Aurora B-INCENP in tight binding, time-dependent manner. Dissociation of this compound from Aurora B-INCENP is slow with at 1/2 of 920 minutes, and the affinity constant for its binding to Aurora B-INCENP is determined to be 0.02 nM. It induces inhibition of cell proliferation in cultured human cancer cell lines from different tissues with IC50s ranging from 40 to 500nM. Consistent with Aurora B inhibition, this chemical treatment produces polyploidy in human PC3 prostate cancer and HL60 acute myeloid leukemia cells as measured by immunofluorescence and flow cytometry. Examination of a broad panel of kinases reveals that multiple kinases, including FLT3, FGFR and the Src family kinases, are inhibited by this agent with IC50 values similar to those for Aurora A and B. In cells, it suppresses the Flt3 and FGFR2 autophosphorylation with IC50 values close to that of Aurora B as measured by cellular histone H3 phosphorylation, whereas the IC50s for inhibition of cellular Src and Bcr Abl are 20-fold weaker. In a panel of pathway specific reporter-based cell models, it inhibits the NFkB and JAK/STAT pathways with submicromolar potency.
References	[1] http://mct.aacrjournals.org/cgi/content/meeting_abstract/8/12_MeetingAbstracts/B270 [2] https://pubmed.ncbi.nlm.nih.gov/23358665/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT00935844	Completed	Advanced Solid Tumors\|Lymphoma	Millennium Pharmaceuticals Inc.	October 2009	Phase 1
NCT00807677	Completed	Acute Myeloid Leukemia\|Acute Lymphoblastic Leukemia\|Chronic Myelogenous Leukemia\|Chronic Lymphocytic Leukemia\|Multiple Myeloma\|Waldenstrom''s Macroglobulinemia\|Myelodysplastic Syndrome\|Philadelphia Chromosome-negative CML\|Myeloid Metaplasia\|Myelofibrosis\|Advanced Polycythemia\|Non-Hodgkins Lymphoma	Millennium Pharmaceuticals Inc.	March 2009	Phase 1

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TAK-901 Aurora Kinase inhibitor

Chemical Structure

Molecular Weight: 504.64