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TAK-901

TAK-901 is a novel inhibitor of Aurora A and Aurora B with IC50 of 21 nM and 15 nM, respectively.

Catalog No.S2718

: Tel: +1-832-582-8158[email protected]

TAK-901 Chemical Structure
Molecular Weight: 504.64

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

TAK-901 is available in the following compound libraries:

Chemical Library (96-well) Inhibitor Library (96-well) Kinase Inhibitor Library (96-well)

Product Information

Compare Aurora Kinase Inhibitors

Research Area
Research Area
Dr. Antonino Maria Sparta demonstrates a breakthrough in leukemia research by utilizing two inhibitors produced by Selleck Chemicals.

Cat.No.	Product Name	Solubility (25°C)
S1133	MLN8237 (Alisertib)	<1 mg/mL	1 mg/mL	<1 mg/mL
S1147	Barasertib (AZD1152-HQPA)	<1 mg/mL	102 mg/mL	3 mg/mL
S1048	VX-680 (MK-0457, Tozasertib)	<1 mg/mL	93 mg/mL	<1 mg/mL
S1107	Danusertib (PHA-739358)	<1 mg/mL	95 mg/mL	<1 mg/mL
S1103	ZM-447439	<1 mg/mL	103 mg/mL	<1 mg/mL
S1249	JNJ-7706621	<1 mg/mL	79 mg/mL	<1 mg/mL
S1100	MLN8054	<1 mg/mL	95 mg/mL	<1 mg/mL
S1134	AT9283	<1 mg/mL	76 mg/mL	38 mg/mL
S2158	KW 2449	<1 mg/mL	67 mg/mL	67 mg/mL
S1529	Hesperadin	<1 mg/mL	103 mg/mL	<1 mg/mL
S2770	MK-5108 (VX-689)	<1 mg/mL	92 mg/mL	<1 mg/mL
S1181	ENMD-2076	1 mg/mL	105 mg/mL	<1 mg/mL
S2725	PF-03814735	<1 mg/mL	0.4 mg/mL	<1 mg/mL
S2740	GSK1070916	<1 mg/mL	102 mg/mL	102 mg/mL
S1154	SNS-314	6 mg/mL	105 mg/mL	<1 mg/mL
S1171	CYC116	<1 mg/mL	24 mg/mL	<1 mg/mL
S1451	Aurora A Inhibitor I	<1 mg/mL	118 mg/mL	<1 mg/mL
S2719	AMG 900	<1 mg/mL	100 mg/mL	<1 mg/mL
S1454	PHA-680632	<1 mg/mL	100 mg/mL	<1 mg/mL
S1519	CCT129202	<1 mg/mL	3 mg/mL	<1 mg/mL
S2718	TAK-901	<1 mg/mL	101 mg/mL	<1 mg/mL
S2744	CCT137690	<1 mg/mL	4 mg/mL	<1 mg/mL

Product Description

Biological Activity Protocol Chemical Information Tech Support & FAQs

Biological Activity

Description	TAK-901 is a novel inhibitor of Aurora A and Aurora B with IC50 of 21 nM and 15 nM, respectively.
Targets	Aurora A-TPX2	Aurora B-INCENP
IC50	21 nM	15 nM ^[1]
In vitro	TAK-901 inhibits Aurora A-TPX2 and Aurora B-INCENP in tight binding, time-dependent manner. Dissociation of TAK-901 from Aurora B-INCENP is slow with at 1/2 of 920 minutes, and the affinity constant for TAK-901 binding to Aurora B-INCENP is determined to be 0.02 nM. TAK-901 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, TAK-901 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 TAK-901 with IC50 values similar to those for Aurora A and B. In cells, TAK-901 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, TAK-901 inhibits the NFkB and JAK/STAT pathways with submicromolar potency. ^[1]
In vivo
Clinical Trials	TAK-901 is now under the Phase 1 clinical trial for the dose escalation in subjects with advanced hematologic malignancies.
Features

Protocol(Only for Reference)

References

Chemical Information

Download TAK-901 SDF

Molecular Weight (MW)	504.64
Formula	C₂₈H₃₂N₄O₃S
CAS No.	934541-31-8, 934542-50-4 (HCl), 1020203-96-6 (Fumaric acid), 1020203-86-4 (benzenesulfonate)
Synonyms	N/A

Solubility (25°C) DMSO 101 mg/mL Water <1 mg/mL Ethanol <1 mg/mL
Storage	2 years -20°CPowder
	2 weeks4°Cin DMSO
	6 months-80°Cin DMSO

Chemical Name	5-(3-(ethylsulfonyl)phenyl)-3,8-dimethyl-N-(1-methylpiperidin-4-yl)-9H-pyrido[2,3-b]indole-7-carboxamide

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Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3Monday–Friday 9:00 AM–5:00 PM (Central Time)

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Related Aurora Kinase Inhibitors

VX-680 (MK-0457, Tozasertib)

VX-680 (MK-0457, Tozasertib) is a pan-Aurora inhibitor of Aurora A, Aurora B and Aurora C with K_i^app of 0.6 nM, 18 nM and 4.6 nM, respectively.
MLN8054

MLN8054 is a potent and selective inhibitor of Aurora A with IC50 of 4 nM.
ZM-447439

ZM-447439 is a selective and ATP-competitive inhibitor for Aurora A and Aurora B with IC50 of 110 nM and 130 nM, respectively.
Danusertib (PHA-739358)

Danusertib (PHA-739358) is an Aurora inhibitor for Aurora A/B/C, Bcr-Abl, c-RET and FGFR with IC50 of 13 nM/79 nM/61 nM, 25 nM, 31 nM and 47 nM, respectively.
MLN8237 (Alisertib)

MLN8237 (Alisertib) is a selective Aurora A inhibitor with IC50 of 1.2 nM.
AT9283

AT9283 is a potent pan-Aurora inhibitor for Aurora A, Aurora B, JAK3, JAK2 and Abl with IC50 of 3 nM, 3 nM, 1.1 nM, 1.2 nM and 4 nM, respectively.
Barasertib (AZD1152-HQPA)

AZD1152-HQPA (Barasertib) is a highly selective Aurora B inhibitor with IC50 of 0.37 nM.
SNS-314

SNS-314 Mesylate is a potent and selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 9 nM, 31 nM, and 3.4 nM, respectively.
CYC116

CYC116 is a potent inhibitor of Aurora A/B and VEGFR with K_i of 8.0 nM/9.2 nM and 44 nM, respectively.
ENMD-2076

ENMD-2076 is a selective inhibitor of Aurora A and Aurora B with IC50 of 14 nM and 350 nM and also inhibits Flt3, Flt4 and VEGFR2 with IC50 of 1.86 nM/15.9 nM and 58.2 nM, respectively.

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TAK-901