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JPM-OEt

Alias: JPM-OEt JPM OEt JPMOEt JPM-565 Ethyl ester
Cat No.:V22994 Purity: ≥98%
JPM-OEt is a broad spectrum (a wide range) inhibitor of cysteine cathepsin.
JPM-OEt
JPM-OEt Chemical Structure CAS No.: 262381-84-0
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
10mg
Other Sizes
Official Supplier of:
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Product Description
JPM-OEt is a broad spectrum (a wide range) inhibitor of cysteine cathepsin. JPM-OEt covalently binds at the active site and irreversibly inhibits the cysteine cathepsin family. Has anti-tumor activity.
Biological Activity I Assay Protocols (From Reference)
ln Vivo
JPM-OEt (50 mg/kg; intraperitoneal injection; once daily for 30 days) effectively lowers tumor cathepsin B activity [1]. JPM-OEt (50 mg/kg; i.p.; twice daily for 4 weeks) causes tumor regression in the RIP1-Tag2 (RT2) animal model of islet cell carcinogenesis [2]. JPM-OEt (50 mg/kg; i.p.; daily for 63 to 98 days) produces a considerable delay in the growth in tumor burden within the first 2 weeks of treatment [3].
Animal Protocol
Animal/Disease Models: Transgenic mice Female mice [3]
Doses: 50 mg/kg
Route of Administration: intraperitoneal (ip) injection; one time/day from 63 to 98 days
Experimental Results: The increase in tumor burden was Dramatically delayed during the first 2 weeks of treatment. However, no significant differences were detected between the two groups on days 84, 91, and 98.
References

[1]. Cathepsin B inhibition limits bone metastasis in breast cancer. Cancer Res. 2012 Mar 1;72(5):1199-209.

[2]. Inhibition of cysteine cathepsin protease activity enhances chemotherapy regimens by decreasing tumor growth and invasiveness in a mouse model of multistage cancer. Cancer Res. 2007 Aug 1;67(15):7378-85.

[3]. Trial of the cysteine cathepsin inhibitor JPM-OEt on early and advanced mammary cancer stages in the MMTV-PyMT-transgenic mouse model. Biol Chem. 2008 Aug;389(8):1067-74.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C20H28N2O6
Molecular Weight
392.4461
Exact Mass
392.195
CAS #
262381-84-0
PubChem CID
11257859
Appearance
White to off-white solid powder
LogP
1.694
Hydrogen Bond Donor Count
3
Hydrogen Bond Acceptor Count
6
Rotatable Bond Count
11
Heavy Atom Count
28
Complexity
545
Defined Atom Stereocenter Count
3
SMILES
CCOC(=O)[C@@H]1[C@H](O1)C(=O)N[C@@H](CC(C)C)C(=O)NCCC2=CC=C(C=C2)O
InChi Key
VRFYYTLIPKHELT-ULQDDVLXSA-N
InChi Code
InChI=1S/C20H28N2O6/c1-4-27-20(26)17-16(28-17)19(25)22-15(11-12(2)3)18(24)21-10-9-13-5-7-14(23)8-6-13/h5-8,12,15-17,23H,4,9-11H2,1-3H3,(H,21,24)(H,22,25)/t15-,16-,17-/m0/s1
Chemical Name
ethyl (2S,3S)-3-(((S)-1-((4-hydroxyphenethyl)amino)-4-methyl-1-oxopentan-2-yl)carbamoyl)oxirane-2-carboxylate
Synonyms
JPM-OEt JPM OEt JPMOEt JPM-565 Ethyl ester
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: This product requires protection from light (avoid light exposure) during transportation and storage.
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 : ~125 mg/mL (~318.51 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 6.25 mg/mL (15.93 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 6.25 mg/mL (15.93 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 6.25 mg/mL (15.93 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 900 μL corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.5481 mL 12.7405 mL 25.4810 mL
5 mM 0.5096 mL 2.5481 mL 5.0962 mL
10 mM 0.2548 mL 1.2740 mL 2.5481 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.

Calculator

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • Enter 5 in the Volume box and choose the correct unit (mL)
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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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)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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.
             (2) Be sure to add the solvent(s) in order.

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