Hesperadin hydrochloride


Catalog No. Size PriceQuantity
M16432-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

Hesperadin hydrochloride is an ATP competitive indolinone inhibitor of Aurora A and B. Hesperadin hydrochloride inhibits Aurora B with an IC50 of 250 nM.

Product information

Molecular Weight: 553.12

Formula: C29H33ClN4O3S

Chemical Name: N-[(3Z)-2-oxo-3-[phenyl({4-[(piperidin-1-yl)methyl]phenyl}amino)methylidene]-2,3-dihydro-1H-indol-5-yl]ethane-1-sulfonamide hydrochloride

Smiles: Cl.CCS(=O)(=O)NC1C=C2/C(=C(/NC3=CC=C(CN4CCCCC4)C=C3)\C3C=CC=CC=3)/C(=O)NC2=CC=1

InChiKey: XMYLEXZLFZAOQN-LXCLTORNSA-N

InChi: InChI=1S/C29H32N4O3S.ClH/c1-2-37(35,36)32-24-15-16-26-25(19-24)27(29(34)31-26)28(22-9-5-3-6-10-22)30-23-13-11-21(12-14-23)20-33-17-7-4-8-18-33;/h3,5-6,9-16,19,30,32H,2,4,7-8,17-18,20H2,1H3,(H,31,34);1H/b28-27-;

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Hesperadin (10-100 nM) inhibits the Aurora kinase-1 (TbAUK1)-mediated phosphoryation of trypanosome histone H3 (TbH3) in a dose dependent manner, with an IC50 of 40 nM. Hesperadin (0.01-10 μM; 24 or 48 hours) inhibits growth of bloodstream forms (BF) and procyclic forms (PF) cultures. Hesperadin (100-200 nM; 24-72 hours) alters cell morphology and inhibits cell cycle progression similar to the RNAi knockdown of TbAUK1.

In Vivo:

Hesperadin (20 mg/kg/d; i.v.) prolongs the survival of xenograft mice via synergistic effect with Temozolomide (TMZ).

Products are for research use only. Not for human use.

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