Description
AZ82 is a selective kinesin-like protein KIFC1 (HSET/KIFC1) inhibitor, with a Ki of 43 nM and an IC50 of 300 nM for KIFC1.
Product information
CAS Number: 1449578-65-7
Molecular Weight: 560.63
Formula: C28H31F3N4O3S
Chemical Name: (2R)-2-[(5-methyl-4-propylthiophen-2-yl)formamido]-N-[(3R)-pyrrolidin-3-yl]-3-{6-[3-(trifluoromethoxy)phenyl]pyridin-3-yl}propanamide
Smiles: CC1SC(=CC=1CCC)C(=O)N[C@H](CC1C=NC(=CC=1)C1=CC(=CC=C1)OC(F)(F)F)C(=O)N[C@H]1CNCC1
InChiKey: PMTLKNOARSHUJB-ZJSXRUAMSA-N
InChi: InChI=1S/C28H31F3N4O3S/c1-3-5-19-14-25(39-17(19)2)27(37)35-24(26(36)34-21-10-11-32-16-21)12-18-8-9-23(33-15-18)20-6-4-7-22(13-20)38-28(29,30)31/h4,6-9,13-15,21,24,32H,3,5,10-12,16H2,1-2H3,(H,34,36)(H,35,37)/t21-,24-/m1/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 125 mg/mL (222.96 mM; Need ultrasonic).
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:
AZ82 is shown to specifically induce multipolar spindles in BT-549 cells, but not in cancer cells with normal centrosome number, such as HeLa. AZ82 binds specifically to KIFC1/MT complex but not to KIFC1 or MT alone. Treatment with AZ82 caused centrosome declustering in BT-549 breast cancer cells with amplified centrosomes. AZ82 inhibits both processes with an IC50 of 0.90 ± 0.09 μM for mant-ATP binding and 1.26 ± 0.51 μM for mant-ADP releasing.
Products are for research use only. Not for human use.
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