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Art. -Nr.: HY-189065

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STF-3600

STF-3600 is a LRRK2^G2019S inhibitor with an IC₅₀ of 0.9 nM against the human target. It has oral activity and can cross the blood-brain barrier. STF-3600 selectively inhibits kinase activity, including autophosphorylation at Ser935 and Ser1292, as well as phosphorylation of the endogenous substrate Rab10 at Thr73. STF-3600 inhibits vacuolization of type II pulmonary epithelial cells in wild-type/heterozygous mice, while it induces this vacuolization phenotype in homozygous mice. STF-3600 can be used in Parkinson's disease research.

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CAS. Nr.: 2765654-79-1
Formel: C₂₄H₂₁N₅
Molecular Weight:379.46

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

STF-3600 Chemical Structure

CAS. Nr.: 2765654-79-1

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

LRRK2^G2019S

0.9 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC50	2.1 nM	Inhibition of pSer935 LRRK2 in HEK293 cells stably expressing human G2019S LRRK2 incubated for 2 hrs measured by CisBio phospho-LRRK2 (Ser935) kit assay. Inhibition of pSer935 LRRK2 in HEK293 cells stably expressing human G2019S LRRK2 incubated for 2 hrs measured by CisBio phospho-LRRK2 (Ser935) kit assay.	42503786
HEK293	IC50	140 nM	Inhibition of pSer935 LRRK2 in HEK293 cells stably expressing human WT LRRK2 incubated for 2 hrs measured by CisBio phospho-LRRK2 (Ser935) kit assay. Inhibition of pSer935 LRRK2 in HEK293 cells stably expressing human WT LRRK2 incubated for 2 hrs measured by CisBio phospho-LRRK2 (Ser935) kit assay.	42503786
HEK293	IC50	2.0 nM	Inhibition of pSer1292 LRRK2 in HEK293 cells stably expressing human G2019S LRRK2 incubated for 2 hrs measured by MSD assay. Inhibition of pSer1292 LRRK2 in HEK293 cells stably expressing human G2019S LRRK2 incubated for 2 hrs measured by MSD assay.	42503786
HEK293	IC50	38 nM	Inhibition of pSer1292 LRRK2 in HEK293 cells stably expressing human WT LRRK2 incubated for 2 hrs measured by MSD assay. Inhibition of pSer1292 LRRK2 in HEK293 cells stably expressing human WT LRRK2 incubated for 2 hrs measured by MSD assay.	42503786
A549	IC50	6 nM	Inhibition of pThr73 Rab10 in human lung epithelial A549 cells expressing G2019S LRRK2 incubated for 2 hrs measured by plate reader assay with acceptor and donor mixes. Inhibition of pThr73 Rab10 in human lung epithelial A549 cells expressing G2019S LRRK2 incubated for 2 hrs measured by plate reader assay with acceptor and donor mixes.	42503786
A549	IC50	41 nM	Inhibition of pThr73 Rab10 in human lung epithelial A549 cells expressing WT LRRK2 incubated for 2 hrs measured by plate reader assay with acceptor and donor mixes. Inhibition of pThr73 Rab10 in human lung epithelial A549 cells expressing WT LRRK2 incubated for 2 hrs measured by plate reader assay with acceptor and donor mixes.	42503786

In Vitro

STF-3600 (2 h) potently inhibits pSer935 in HEK293 cells expressing LRRK2^G2019S, with an IC₅₀ of 2.1 nM^[1].
STF-3600 (2 h) potently inhibits pSer1292 in HEK293 cells expressing LRRK2^G2019S, with an IC₅₀ of 2 nM^[1].
STF-3600 (2 h) inhibits pThr73 Rab10 in A549 cells expressing LRRK2^G2019S, with an IC₅₀ of 6 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Parmacokinetics

Species	Dose	Route	C_max	T_1/2	MRT	CL	T_max	Bioavailability	Plasma Concentration	Brain Concentration
Mice^[1]	0.5 mg/kg	i.v.	1240 μM	1.24 h	1.46 h	23.5 mL/min/kg	/	/	/	/
Mice^[1]	5 mg/kg	p.o.	1040 μM	/	5.06 h	/	1.0 h	28.7 %	/	/
Mice^[1]	61.6 mg/kg	p.o.	/	/	/	/	/	/	5.02 μM	1.64 μM

In Vivo

STF-3600 (3-100 mg/kg; p.o.; single administration) potently inhibits LRRK2^G2019S in homozygous knock-in mice^[1].
STF-3600 (100 mg/kg/day; oral administration; daily dosing for 21 consecutive days) inhibits LRRK2^G2019S in the brain tissues of heterozygous and homozygous knock-in mice. It does not induce pulmonary toxicity in wild-type or heterozygous mice, but causes pulmonary vacuolization in homozygous knock-in mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

C57BL/6J mice (male and female, 5-8 months old; wild-type, heterozygous G2019S LRRK2 knock-in, and homozygous G2019S LRRK2 knock-in)^[1]
Dosage:

3 mg/kg; 10 mg/kg; 30 mg/kg; 100 mg/kg
Administration:

p.o.; single dose
Result:

Achieved maximal inhibition of pSer935 LRRK2 at 10 mg/kg in homozygous G2019S LRRK2 knock-in mouse brain and lung.
Left pSer935 LRRK2 still detectable at 100 mg/kg in wild-type mice.
Showed greater potency of pThr73 Rab10 inhibition in lung tissue of homozygous G2019S LRRK2 knock-in mice compared to wild-type mice.
Left total LRRK2 and Rab10 levels unchanged in all tissues.

Animal Model:

C57BL/6J mice (male and female, 5-8 months old; wild-type, heterozygous G2019S LRRK2 knock-in, and homozygous G2019S LRRK2 knock-in)^[1]
Dosage:

100 mg/kg/day (actual average exposure 61.6 mg/kg/day)
Administration:

p.o.; daily; 21 days
Result:

Induced overt type II pneumocyte vacuolization in homozygous G2019S LRRK2 knock-in mice (112 vacuolated cells per scanned area), with no vacuolization in wild-type or heterozygous G2019S LRRK2 knock-in mice.
Reduced pSer935 LRRK2 activity to ~15% of vehicle-treated levels in homozygous knock-in mouse brain and ~50% of vehicle-treated levels in heterozygous knock-in mouse brain, with no significant effect in wild-type mouse brain.
Caused no significant changes in complete blood count measures across any genotype or gender.

Chemical Information

CAS. Nr. 2765654-79-1
Molecular Weight 379.46
Formel C₂₄H₂₁N₅
SMILES

CC1=CC(C2=NNC3=CC=C(C=C23)N[C@@H]4C5=CC=C(C#N)C=C5CCC4)=CC=N1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Garofalo AW, et al. G2019S LRRK2 Kinase Inhibition in Heterozygous Mice Avoids Lung Phenotype Observed with Inhibition of WT LRRK2. ACS chemical neuroscience. 2026 Aug 05;17(15):2982-2990.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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