Fadraciclib (CYC065)

Catalog No.S7371 Batch:S737101

Technical Data

Formula	C₂₁H₃₁N₇O
Molecular Weight	397.52	CAS No.	1070790-89-4
Solubility (25°C)*	In vitro	DMSO	80 mg/mL (201.24 mM)
		Ethanol	80 mg/mL (201.24 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.)

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Biological Activity

Description

Fadraciclib (CYC065) is a novel, orally available ATP-competitive inhibitor of CDK2/CDK9 kinases with IC50 of 5 nM and 26 nM, respectively.

Targets

CDK2 ^[1]	CDK9 ^[1]
5 nM	26 nM

In vitro

Fadraciclib effectively downregulates pro-survival and leukemogenic proteins and that short pulse treatment is sufficient to substantially decrease cell viability of the majority of AML cell lines tested via apoptotic induction.<a class="sref" href="#s_ref">[1]</a>

In vivo

Fadraciclib shows potent anti-leukemic activity in two subcutaneous xenograft models EOL-1 (with MLL-PTD) and HL60 (non MLLr/MLL-PTD AML with MYC amplification).<a class="sref" href="#s_ref">[1]</a>

Protocol (from reference)

Cell Assay:^{<sup><a class="sref" href="#s_ref">[2]</a></sup>}	Cell lines AML cell lines Concentrations 1 μM Incubation Time 72 h Method Half-maximal inhibitory concentration (IC50) of AML cell lines treated with fadraciclib for up to 72 h was established using 7-Hydroxy-3H-phenoxazin-3-one-10-oxide sodium salt resazurin assay according to manufacturer’s instructions. IC50 were calculated using GraphPad Prism 8 software (GraphPad Software).
Animal Study:^{<sup><a class="sref" href="#s_ref">[1]</a></sup>}	Animal Models Female athymic CB-17 SCID (Harlan Sprague-Dawley) mice Dosages 40 or 55 mg/kg Administration Oral gavage

Cell Assay:^{<a class="sref" href="#s_ref">[2]</a>}

Cell lines
AML cell lines
Concentrations
1 μM
Incubation Time
72 h
Method
Half-maximal inhibitory concentration (IC50) of AML cell lines treated with fadraciclib for up to 72 h was established using 7-Hydroxy-3H-phenoxazin-3-one-10-oxide sodium salt resazurin assay according to manufacturer’s instructions. IC50 were calculated using GraphPad Prism 8 software (GraphPad Software).

Animal Study:^{<a class="sref" href="#s_ref">[1]</a>}

Animal Models
Female athymic CB-17 SCID (Harlan Sprague-Dawley) mice
Dosages
40 or 55 mg/kg
Administration
Oral gavage

References

Selleck's Fadraciclib (CYC065) has been cited by 1 publication

Cyclin-dependent kinase inhibitors enhance programmed cell death protein 1 immune checkpoint blockade efficacy in triple-negative breast cancer by affecting the immune microenvironment [ Cancer, 2024, 130(S8):1449-1463]	PubMed: 38482921

Cyclin-dependent kinase inhibitors enhance programmed cell death protein 1 immune checkpoint blockade efficacy in triple-negative breast cancer by affecting the immune microenvironment [ Cancer, 2024, 130(S8):1449-1463]

PubMed: 38482921

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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.

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