VPS34 inhibitor 1

Alias: Vps34-IN1; Compound 19; PIK-III analogue
Cat No.:V0985 Purity: ≥98%
VPS34 inhibitor 1 (also known as Vps34-IN1, Compound 19, PIK-III analogue) is a potent and selective inhibitor of VPS34 the potential to serve as a chemical tool to modulate autophagy in Vivo.
VPS34 inhibitor 1 Chemical Structure CAS No.: 1383716-46-8
Product category: PI3K
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

VPS34 inhibitor 1 (also known as Vps34-IN1, Compound 19, PIK-III analogue) is a potent and selective inhibitor of VPS34 the potential to serve as a chemical tool to modulate autophagy in Vivo. It inhibits VPS34 with an IC50 of 15 nM. VPS34 inhibitor 1 does not significantly inhibit the activity of over 340 additional kinases, including class I and II PI3Ks. Vps34-IN1 induces a rapid dose-dependent dispersal of a specific PtdIns-(3)-P-binding probe from endosome membranes, within one minute, without affecting the ability of class I PI3K to regulate Akt.

Biological Activity I Assay Protocols (From Reference)
Targets
VPS34 (IC50 = 15 nM)
ln Vitro
Compound 19 is extraordinarily selective over other lipid and protein kinases. Compound 19 and PIK-III have comparable abilities to stop the breakdown of the autophagy substrates p62, NCOA4, NBR1, NDP52, and FTH1. Additionally, compound 19 causes cells to produce more lipidated and nonlipidated forms of LC3, which is consistent with earlier studies using PIK-III[1].
ln Vivo
The pharmacokinetic profile of analogue 19 is determined in C57BL/6 mice. Oral administration of the compound at a dose of 10 mg/kg results in rapid absorption, moderate mean systemic clearance (30 mL/min/kg, or roughly 33% of hepatic blood flow), and good oral bioavailability (F% = 47). Compound 19 qualifies as a suitable candidate for in vivo studies based on these PK parameters and the cellular activity. When compound 19 is given orally twice daily (BID) at a dose of 50 mg/kg for seven days, LC3-II builds up in a way that is time-dependently consistent with decreased autophagic capacity. It prevents autophagy in living cells[1].
Cell Assay
For inhibitor assay, cells are plated and the following day when cells had reached 90%, are treated with dimethyl sulfoxide (DMSO, vehicle) or the indicated concentration of PIK-III or Compound 19, both dissolved in DMSO. After 24 hours, cells are lysed in RIPA supplemented with 1% SDS and mini-EDTA protease inhibitors, homogenized by passage through a Qiashredder column, and the protein is quantified by DC Lowry protein assay.
Animal Protocol
C57BL/6 Mice
10 mg/kg(p.o.) or 2 mg/kg(I.V.)
oral administration or I.V.
References

[1]. ACS Med Chem Lett. 2015 Nov 13;7(1):72-6.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C21H25N7O
Molecular Weight
391.47
CAS #
1383716-46-8
Appearance
Solid
SMILES
CC(C)(CNC1=NC=C(C(=N1)CC2CC2)C3=NC(=NC=C3)NC4=CC=NC=C4)O
InChi Key
CC(C)(CNC1=NC=C(C(=N1)CC2CC2)C3=NC(=NC=C3)NC4=CC=NC=C4)O
InChi Code
XJTIGGCBXFIZJV-UHFFFAOYSA-N
Chemical Name
1-[[4-(cyclopropylmethyl)-5-[2-(pyridin-4-ylamino)pyrimidin-4-yl]pyrimidin-2-yl]amino]-2-methylpropan-2-ol
Synonyms
Vps34-IN1; Compound 19; PIK-III analogue
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~78 mg/mL (199.2 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.5545 mL 12.7724 mL 25.5447 mL
5 mM 0.5109 mL 2.5545 mL 5.1089 mL
10 mM 0.2554 mL 1.2772 mL 2.5545 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Biological Data
  • VPS34 inhibitor 1 (Compound 19, PIK-III analogue)

  • VPS34 inhibitor 1 (Compound 19, PIK-III analogue)
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