ChemicalBook CAS DataBase List 2375554-02-0

2375554-02-0

Name	Senexin C
CAS	2375554-02-0
Molecular Formula	C28H27N5O
Molecular Weight	449.56
MOL File	2375554-02-0.mol

Chemical Properties

form	Solid
color	Off-white to light yellow

Hazard Information

Description

Senexin C exhibits potent CDK8/19 inhibitory activity with high selectivity. Senexin C is more metabolically stable and provides a more sustained inhibition of CDK8/19-dependent cellular gene expression when compared with the prototype inhibitor Senexin B. Senexin C inhibits MV4-11 leukemia growth in a systemic in vivo model with good tolerability.

Uses

Senexin C is a selective and orally active CDK8/19 inhibitor. Senexin C shows a strong tumor-enrichment pharmacokinetic (PK) profile and tumor-pharmacodynamic (PD) marker responses. Senexin C inhibits the growth of MV4-11 leukemia cells with good tolerability[1].

in vivo

Senexin C (2.5 mg/kg, i.v.; 100 mg/kg, p.o.) shows good oral bioavailability^[1].
Senexin C (40 mg/kg; p.o.; twice daily for 4 weeks) suppresses the systemic growth of MV4-11 AML with good tolerability^[1]. Pharmacokinetic Parameters of Senexin C in eight-week-old female Balb/c mice^[1].

parameters	iv (2.5 mg/kg)	po (100 mg/kg)
	plasma	tumor	plasma	tumor
C₀ (μg/mL)	503
K_el (h^-1)	0.93	0.06	0.2	0.1
T_1/2 (h)	0.75	12.1	3.53	7.27
T_max (h)		0.58	12	12
C_max (ng/mL or ng/g)		488	144	5728
AUC0-24 h (ng x h/ml or ng x h/g)	331	6408	2182	88,600
F%			16.5%	34.6%

Eight-week-old female Balb/c mice ( CT26 tumor mode), 2.5 mg/kg, i.v.(2.5 mg/mL Senexin C solution in 5% dextrose); 100 mg/kg, p.o.(10 mg/mL Senexin C solution in 30% propylene glycol/70% PEG-400 vehicle)^[1].

Animal Model:	eight-week-old female Balb/c mice ( CT26 tumor mode)^[1]
Dosage:	2.5 mg/kg (10 mL/kg of 2.5 mg/mL Senexin C solution in 5% dextrose), 100 mg/kg (10 mL/kg of 10 mg/mL Senexin C solution in 30% propylene glycol/70% PEG-400 vehicle)
Administration:	2.5 mg/kg, i.v.; 100 mg/kg, p.o.
Result:	Showed good oral bioavailability.

Animal Model:	eight-week-old female NSG mice ( AML model)^[1]
Dosage:	40 mg/kg
Administration:	p.o.; twice daily, 4 weeks
Result:	Suppressed the systemic growth of MV4-11 AML with good tolerability.

IC 50

CDK8/CycC: 3.6 nM (IC₅₀); CDK19/CycC: 2.9 nM (Kd); CDK8/CycC: 1.4 nM (Kd)

References

[1] Zhang L, et al. A Selective and Orally Bioavailable Quinoline-6-Carbonitrile-Based Inhibitor of CDK8/19 Mediator Kinase with Tumor-Enriched Pharmacokinetics. J Med Chem. 2022; 65(4):3420-3433. DOI:10.1021/acs.jmedchem.1c01951

Spectrum Detail

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