SKLB-23bb

Catalog No.S8743 Batch:S874301

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Technical Data

Formula

C21H24N4O4
Molecular Weight 396.44 CAS No. 1815580-06-3
Solubility (25°C)* In vitro DMSO 79 mg/mL (199.27 mM)
Ethanol 79 mg/mL (199.27 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

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.
Targets
HDAC6 [1]
(Cell-based assay)
<100 nM
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[1].
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[1].

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    HCT116 and A2780S cells

  • Concentrations

    200 nM

  • Incubation Time

    3, 6, 12 and 24 h

  • Method

    --
Animal Study:

[1]
  • Animal Models

    HCT116, A2780S, and MCF-7 xenografts established on Balb/c nude mice

  • Dosages

    3, 6, 12.5, 25 and 50 mg/kg

  • Administration

    oral

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.