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LAT1-IN-1

Cat No.:V31880 Purity: ≥98%
BCH (2-Amino-2-norbornanecarboxylic acid) is a selective competitive inhibitor of L-type amino acid (AA) transporter 1 (LAT1).
LAT1-IN-1
LAT1-IN-1 Chemical Structure CAS No.: 20448-79-7
Product category: New2
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
50mg
100mg
Other Sizes
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Product Description
BCH (2-Amino-2-norbornanecarboxylic acid) is a selective competitive inhibitor of L-type amino acid (AA) transporter 1 (LAT1). It can significantly inhibit cellular uptake of amino acid (AA)s and mTOR phosphorylation, thereby inhibiting cancer/tumor cell growth and inducing cell Apoptosis.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
The application of BCH (1-100 mM; 3 days) to esophageal cancer cells (KYSE30 and KYSE150) exhibited dose-dependent inhibition of cell growth [1]. The number of G0/G1 phase cells in KYSE30 and KYSE150 cells was considerably enhanced by BCH (30 mM; 24 and 48 hours); this suggests that BCH induces cell cycle arrest in the G1 phase [1]. After 30 minutes, the phosphorylation of 4E-BP1 and p70S6K was reduced by BCH (30 mM; 0-24 h; KYSE30 and KYSE150 cells), and this reduction lasted for 24 hours. Protein levels of mTOR, 4E-BP1, and p70S6K are marginally decreased [1].
ln Vivo
The treatment of male BALB/c nude mice with BCH (200 mg/kg; intravenous injection; daily; for 14 days) significantly delayed the growth of the tumor and decreased glucose metabolism, indicating that LAT1 inhibition may prevent the growth of esophageal cancer in vivo [1].
Cell Assay
Cell Proliferation Assay[1]
Cell Types: KYSE30 and KYSE150 Esophageal cancer cells
Tested Concentrations: 1 mM, 3 mM, 5 mM, 10 mM, 20 mM, 30 mM, 40 mM, 50 mM or 100 mM
Incubation Duration: 3 days
Experimental Results: Cell proliferation was inhibited in a dose-dependent manner.

Cell cycle analysis[1]
Cell Types: KYSE30 and KYSE150 Cell
Tested Concentrations: 30 mM
Incubation Duration: 24 and 48 hrs (hours)
Experimental Results: Cell cycle arrest.

Western Blot Analysis [1]
Cell Types: KYSE30 and KYSE150 Cell
Tested Concentrations: 30 mM
Incubation Duration: 0 hrs (hours), 0.5 hrs (hours), 1 hour, 3 hrs (hours), 6 hrs (hours), 24 hrs (hours)
Experimental Results: diminished phosphorylation of 4E-BP1 and p70S6K. The amounts of mTOR, 4E-BP1 and p70S6K proteins were slightly diminished.
Animal Protocol
Animal/Disease Models: Male BALB/c nude mice (5 weeks old) KYSE150 cells [1]
Doses: 200 mg/kg
Route of Administration: intravenous (iv) (iv)injection; daily; continued for 14 days
Experimental Results: Dramatically delayed tumor growth and diminished glucose metabolism.
References

[1]. Efficacy of system l amino acid transporter 1 inhibition as a therapeutic target in esophageal squamous cell carcinoma. Cancer Sci. 2016 Oct;107(10):1499-1505.

[2]. Discovery of Potent Inhibitors for the Large Neutral Amino Acid Transporter 1 (LAT1) by Structure-Based Methods. Int J Mol Sci. 2018 Dec 21;20(1).

[3]. L-type amino acid transport and cancer: targeting the mTORC1 pathway to inhibit neoplasia. Am J Cancer Res. 2015 Mar 15;5(4):1281-94. eCollection 2015.

Additional Infomation
2-Amino-2-norbornanecarboxylic acid is a monoterpenoid.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C8H13NO2
Molecular Weight
155.19432
Exact Mass
155.095
CAS #
20448-79-7
PubChem CID
115288
Appearance
White to off-white solid powder
Density
1.256g/cm3
Boiling Point
295.5ºC at 760 mmHg
Melting Point
>300 °C(lit.)
Flash Point
132.5ºC
Vapour Pressure
0.000369mmHg at 25°C
Index of Refraction
1.559
LogP
1.288
Hydrogen Bond Donor Count
2
Hydrogen Bond Acceptor Count
3
Rotatable Bond Count
1
Heavy Atom Count
11
Complexity
204
Defined Atom Stereocenter Count
0
InChi Key
MPUVBVXDFRDIPT-UHFFFAOYSA-N
InChi Code
InChI=1S/C8H13NO2/c9-8(7(10)11)4-5-1-2-6(8)3-5/h5-6H,1-4,9H2,(H,10,11)
Chemical Name
2-aminobicyclo[2.2.1]heptane-2-carboxylic acid
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
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)
H2O : ~20 mg/mL (~128.87 mM)
DMSO : ~1 mg/mL (~6.44 mM)
Solubility (In Vivo)
Solubility in Formulation 1: 12.5 mg/mL (80.55 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 6.4437 mL 32.2186 mL 64.4371 mL
5 mM 1.2887 mL 6.4437 mL 12.8874 mL
10 mM 0.6444 mL 3.2219 mL 6.4437 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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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

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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