CDKI-73

Catalog No.S7773 Batch:S777302

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Technical Data

Formula

C15H15FN6O2S2
Molecular Weight 394.45 CAS No. 1421693-22-2
Solubility (25°C)* In vitro DMSO 50 mg/mL (126.75 mM)
Water Insoluble
Ethanol 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 CDKI-73 (LS-007) is a potent CDK inhibitor in vitro with IC50 of 8.17 nM, 3.27 nM, 8.18 nM, and 5.78 nM for CDK1, CDK2, CDK4, and CDK9, respectively. CDKI-73 induces apoptosis in cancer cells. CDKI-73 is an orally bioavailable and highly efficacious CDK9 inhibitor against acute myeloid leukemia.
Targets
CDK2 [1]
(Cell-free assay)		 CDK9 [1]
(Cell-free assay)		 CDK1 [1]
(Cell-free assay)		 CDK4 [1]
(Cell-free assay)
3.27 nM 5.78 nM 8.17 nM 8.18 nM
In vitro

CDKI-73 induces cancer cells undergoing apoptosis through transcriptional downregulation of anti-apoptotic proteins Bcl-2, Mcl-1 and XIAP by majorly targeting CDK9. Contrastively, it is relatively low toxic to the bone marrow cells of healthy donors.[2]
In vivo

CDKI-73 is orally bioavailable, highly efficacious against MLL-AML MV4–11 xenografts and downregulates anti-apoptotic proteins by targeting CDK9 in vivo.[2]

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    Leukemia cell lines (MOLM13, MV4-11, THP-1, etc.)

  • Concentrations

    0.05 μM, 0.1 μM, 0.25 μM, 0.5 μM

  • Incubation Time

    1 h, 4 h, 12 h, 24 h, 48 h

  • Method

    MV4-11 (1 × 105/well) cells are seeded and incubated under 5% CO2 at 37ºC overnight. After incubation with indicated concentrations of the CDKI-73 for 24 or 48 h, cells are collected and centrifuged (300 g, 5 min). For cell cycle assay, the pellets are re-suspended in cold 70% ethanol and fixed on ice for 15 min, followed by centrifugation (300 g, 5 min). The collected pellets are incubated with 200 μL staining solution at 37ºC for 1 h, then analyzed with a Gallios flow cytometer. Apoptosis is assessed with cells collected and processed as per the instruction in the annexin V-FITC/PI commercial kit.
Animal Study:

[2]
  • Animal Models

    female nude (nu/nu) Balb/C mice aged 6–8 weeks

  • Dosages

    25 mg/kg

  • Administration

    Oral gavage

Selleck's CDKI-73 has been cited by 1 publication

pH-Responsive Poly(ethylene glycol)-b-poly(2-vinylpyridine) Micelles for the Triggered Release of Therapeutics [ Pharmaceutics, 2023, 15(3)977] PubMed: 36986838

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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.