CDKI-73

Catalog No.S7773 Batch:S777302

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

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

References

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

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

PubMed: 36986838

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

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.