Description
SKLB-23bb is an orally bioavailable HDAC6-selective inhibitor with IC50 values under 100 nmol/L, against most of the cell lines checked. It also has microtubule-disrupting ability.
Product information
CAS Number: 1815580-06-3
Molecular Weight: 396.44
Formula: C21H24N4O4
Chemical Name: N-hydroxy-4-{2-methoxy-5-[methyl(2-methylquinazolin-4-yl)amino]phenoxy}butanamide
Smiles: CC1N=C(C2=CC=CC=C2N=1)N(C)C1=CC(OCCCC(=O)NO)=C(C=C1)OC
InChiKey: FWXZZFONXWYSEF-UHFFFAOYSA-N
InChi: InChI=1S/C21H24N4O4/c1-14-22-17-8-5-4-7-16(17)21(23-14)25(2)15-10-11-18(28-3)19(13-15)29-12-6-9-20(26)24-27/h4-5,7-8,10-11,13,27H,6,9,12H2,1-3H3,(H,24,26)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Solubility (25°C). 79 mg/mL(199.27 mM). Insoluble.
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:
SKLB-23bb shows cytotoxic effects against a panel of solid and hematologic tumor cell lines at the low submicromolar level. In contrast to the reported HDAC6-selective inhibitors, SKLB-23bb is more efficient against solid tumor cells. SKLB-23bb selectively inhibits cellular HDAC6, but the antitumor activity of SKLB-23bb is independent of HDAC6. SKLB-23bb could bind to the colchicine site in β-tubulin and act as a microtubule polymerization inhibitor. It blocks tumor cell cycle at G2-M phase and triggers cellular apoptosis.
In Vivo:
In solid tumor xenografts, oral administration of SKLB-23bb efficiently inhibits tumor growth. SKLB-23bb has good pharmacokinetic profiles and is orally bioavailable.
Products are for research use only. Not for human use.
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