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Nanvuranlat (JPH203)

Name: Nanvuranlat (JPH203)
Brand: Selleck Chemicals
SKU: S8667
Rating: 5 (19 reviews)

Synonyms: KYT-0353, JPH-203SBECD

Catalog No.S8667 Purity:99.73%

Nanvuranlat (JPH203, KYT-0353, JPH-203SBECD), a selective L-type amino acid transporter 1 inhibitor, shows a dramatic inhibition of leucine uptake (IC50=0.06 µM) and cell growth (IC50=4.1 µM) in human colon cancer cells (HT-29), human oral cancer cells (YD-38) and leukemic cells.

Nanvuranlat (JPH203) Chemical Structure

CAS No. 1037592-40-7

Purity & Quality Control

Batch: Purity: 99.73%

99.73

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Cell Data

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
HT-29	Function assay	1 hr	Inhibition of [14C]-L-leucine uptake at LAT1 in human HT-29 cells after 1 hr by liquid scintillation counting, IC50=0.06μM.	27253989
YD-38	Function assay	1 hr	Inhibition of [14C]-L-leucine uptake at LAT1 in human YD-38 cells after 1 hr by liquid scintillation counting, IC50=0.79μM.	27253989
HT-29	Growth inhibition assay	96 hrs	Growth inhibition of human HT-29 cells measured after 96 hrs by Coulter counter based cell counting method, IC50=4.1μM.	27253989
Click to View More Cell Line Experimental Data

Biological Activity

Description

Targets

LAT1 ^[1]
(Cell-free assay)

In vitro
In vitro	JPH203 completely and slightly inhibited the L-Leucine uptake in YD-38 cells (IC50 value: 0.79 μM) and NHOKs (IC50 value: >100 μM), respectively. JPH203 inhibited HT-29 cell growth, generating an apparent IC50 of 4.1 μM, but the JPH203 IC50 concentration (0.06 μM) needed to inhibit the L-Leucine uptake did not inhibit HT-29 cell growth, which represents a 68-fold difference in susceptibility^[1]. JPH203 activated the mitochondria-dependent apoptotic signaling pathway by upregulating pro-apoptotic factors, such as Bad, Bax, and Bak, and the active form of caspase-9, and downregulating anti-apoptotic factors, such as Bcl-2 and Bcl-xL in Saos2 human osteosarcoma cells. JPH203 can distinguish relative abundance between LAT1 and LAT2. It has high selectivity for LAT1^[2]. JPH203 was metabolically stable in mouse, rat, dog, monkey and human liver microsomal incubations^[3]. JPH203 induces both G2/M and G0/G1 cell cycle arrest, as well as reduced the S phase accompanied by altered expression of the proteins in cell cycle progression: cyclin D1, CDK4, and CDK6^[4].
Cell Research	Cell lines	Saos2 human osteosarcoma cells
	Concentrations	100 µM
	Incubation Time	72 h
	Method	Colony formation assays are performed by seeding 300 cells/well into 6 well plates. After 24 h of growth, the cells are treated with 100 µM JPH203 for 72 h. The JPH203 treatment is removed and fresh medium is added. The cells are incubated for 10 days. Thereafter, medium is removed and the cells are washed with phosphate buffered saline (PBS) and fixed with 4% paraformaldehyde for 10 min at 4℃. Sequentially, the colonies are stained with 2% crystal violet for 10 min. Finally, colonies stained by crystal violet are washed with PBS and dried at room temperature, before imaged by a digital camera.
Experimental Result Images	Methods	Biomarkers	Images	PMID
	Western blot	p53 / Bad / Bcl-2 / Bcl-xl / Bax / Bak / Cleaved caspase / Cleaved PARP p70S6K / p-P70S6k / p-S6 / S6 / p-ERK / ERK / p-AKT / AKT' p-GCN2 / GCN2 / p-EIF2α / EIF2α / ATF4		29200902
	Growth inhibition assay	Cell viability		29200902

In Vivo
In vivo	Daily intravenous administration of JPH203 (12.5 and 25 mg/kg) significantly inhibited tumor growth in KKU-213 cholangiocarcinoma cell xenografts in the nude mice model in a dose-dependent manner with no statistically significant change in the animal’s body weight and with no differences in the histology and appearance of the internal organs compared with the control group. Thus, JPH203 shows anti-tumor efficacy in nude mice bearing human cholangiocarcinom (CCA) cell xenografts without general toxicity^[4].
Animal Research	Animal Models	Sprague-Dawley rats
	Dosages	0.9-1.0 mg/kg
	Administration	i.v.

References

[4] Yothaisong S, et al. Tumour Biol. 2017, 39(3):1010428317694545.

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Chemical Information & Solubility

Molecular Weight	472.32	Formula	C₂₃H₁₉Cl₂N₃O₄
CAS No.	1037592-40-7	SDF	Download Nanvuranlat (JPH203) SDF
Smiles	C1=CC=C(C=C1)C2=NC3=CC(=CC(=C3O2)COC4=C(C=C(C=C4Cl)CC(C(=O)O)N)Cl)N
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

5%TFA : 2.31 mg/mL

DMSO : 0.01 mg/mL ( (0.02 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.					In vivo Formulation Calculator
	Clear solution	5%DMSO 1 Corn oil	0.15mg/ml (0.32mM)	Taking the 1 mL working solution as an example, add 50 μL of 3 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.	In vivo Formulation Calculator
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	1.18mg/ml (2.50mM)	Taking the 1 mL working solution as an example, add 50 μL of clarified DMSO stock solution of 23.5 mg/ml to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL of ddH2O to make it clear. Volume up to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	2%DMSO 1 98%Corn oil	0.42mg/ml (0.89mM)	Taking the 1 mL working solution as an example, add 20 μL of 21 mg/ml clear DMSO stock solution to 980 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
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