ZT-12-037-01

Catalog No.S8864 Batch:S886401

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Technical Data

Formula

C21H31N5O2
Molecular Weight 385.50 CAS No. 2328073-61-4
Solubility (25°C)* In vitro DMSO 41 mg/mL (106.35 mM)
Ethanol 3 mg/mL (7.78 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 ZT-12-037-01 is a specific and ATP-competitive STK19 inhibitor with IC50s of 23.96 nM and 27.94 nM for STK19 (WT) and STK19 (D89N), respectively. It displays extremely high kinase selectivity using KINOMEscan against a panel of 468 diverse kinases using an in vitro ATP-site competition binding assay at 1 μM.
Targets
STK19 [1]
(Cell-free assay)		 STK19 (D89N) [1]
(Cell-free assay)
23.96 nM 27.94 nM
In vitro

ZT-12-037-01 treatment efficiently inhibits phosphorylation of NRAS in a dose- and time-dependent manner. Furthermore, with increasing ATP concentrations, the IC50 of ZT-12-037-01 against STK19 accordingly increased, indicating that ZT-12-037-01 is an ATP-competitive inhibitor for STK19. ZT-12-037-01 treatment significantly inhibits mutant NRAS-STK19-driven melanocyte colony formation, proliferation, and tumor formation. Pro-apoptotic effect of ZT-12-037-01 is dramatically enhanced in cells expressing oncogenic NRAS[1].
In vivo

ZT-12-037-01 is a highly potent STK19 inhibitor with low in vivo toxicity. Its treatment also inhibits growth of SK-MEL-2 xenograft melanoma (with NRASQ61R) in a dose-dependent manner[1].

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    A375, UACC62, SK-MEL-2 and WM2032 cells

  • Concentrations

    0 μM, 1 μM, or 3 μM

  • Incubation Time

    4 days

  • Method

    --
Animal Study:

[1]
  • Animal Models

    C57BL/6J mice

  • Dosages

    25 mg/kg

  • Administration

    IP

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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.