HSP90-IN-9

Product NameHSP90-IN-9
CAS2765247-36-5
MFC30H31N3O5
MW513.59
EINECS
MOL File2765247-36-5.mol

Chemical Properties

Boiling point	694.009±55.00 °C(Press: 760.00 Torr)(predicted)
Density	1.257±0.06 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted)
pka	8.205±0.50(predicted)

Usage And Synthesis

Uses

HSP90-IN-9 is a potent and selective HSP90 inhibitor. HSP90-IN-9 displays a fungicidal effect in a dose-dependent manner. HSP90-IN-9 inhibits fungal biofilm formation and fungal morphological changes after being combined with FLC. HSP90-IN-9 recovers FLC resistance by down-regulating the expression of related genes (ERG11, CDR1 and CDR2)[1].

in vivo

HSP90-IN-9 (10 mg/kg; i.v.) exhibits moderate pharmacokinetic properties in SD rats^[1].
HSP90-IN-9 (A17 (10 mg/kg)+FLC (1 mg/kg); i.p.; once a day for 5 days) exhibits potent in vivo antifungal efficacy by reducing the colonization and dissemination of fungi in tissue^[1].
Pharmacokinetic Parameters of HSP90-IN-9 in male Sprague-Dawley (SD) rats^[1].

dose (mg/kg)	T_1/2 (h)	C₀ (ng/mL)	AUC_(0-t) (h*ng/mL)	AUC_(0-∞) (h*ng/mL)	V_z (L/kg)	Cl (mL/min/kg)	MRT_(0-∞) (h)
10 mg/kg	1.26±0.31	4752.50±44.54	3005.15±35.59	3028.95±54.14	11.25±3.69	101.77±1.96	1.12±0.07

male Sprague-Dawley (SD) rats; 10 mg/kg; i.v.^[1]

Animal Model:	male Sprague-Dawley (SD) rats^[1]
Dosage:	10 mg/kg
Administration:	i.v.
Result:	Exhibited moderate pharmacokinetic properties in SD rats.

Animal Model:	female SD rats, 160-180 g (IFI rat model)^[1]
Dosage:	10 mg/kg, A17 (10 mg/kg)+FLC (1 mg/kg)
Administration:	i.p., once a day, 5 days
Result:	Exhibited potent in vivo antifungal efficacy by reducing the colonization and dissemination of fungi in tissue.

IC 50

HSP90

References

[1] Yin W, et al. Species-Selective Targeting of Fungal Hsp90: Design, Synthesis, and Evaluation of Novel 4,5-Diarylisoxazole Derivatives for the Combination Treatment of Azole-Resistant Candidiasis. J Med Chem. 2022, 65(7):5539-5564. DOI:10.1021/acs.jmedchem.1c01991

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