| Size | Price | Stock | Qty |
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| 1mg |
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KMH-233 is a potent and selective LAT1 Inhibitor 1. KMH-233 inhibited the uptake of LAT1 substrate, L-leucin as well as cell growth. It also significantly potentiated the efficacy of bestatin and cisplatin even at low concentrations (25 μM). KMH-233 may be a promising agent or adjuvant especially for the treatment of prostate cancer.
| ln Vitro |
By blocking the binding and transport of necessary neutral amino acids, KMH-233 can stop cancer cells from growing [1]. KMH-233 exhibits a noteworthy decrease in cell proliferation, with an IC50 of 124 µM[1]. KMH-233 inhibits cell growth by 53% and 50%, respectively, and is an effective supplement that can boost the anti-proliferative activity of Bestatin (100 µM) and cisplatin (100 µM) at a lower dose of 25 µM[1].
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: MCF-7 Cell Tested Concentrations: 0.5-1000 μM Incubation Duration: 72 hrs (hours) Experimental Results: demonstrated significant reduction in cell growth with IC50 of 124 μM. |
| References |
| Molecular Formula |
C32H25N7O5
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|---|---|
| Molecular Weight |
587.584806203842
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| Exact Mass |
587.191
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| CAS # |
1941174-13-5
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| Related CAS # |
(R)-KMH-233
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| PubChem CID |
154730690
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
2
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
44
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| Complexity |
1160
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CNC(=O)COC1=CC=C(C=C1)C2=C(C3=NC4=CC=CC=C4N3C(=C2C#N)NC(=O)C5=CC=CC(=C5)C[C@@H](C(=O)O)N)C#N
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| InChi Key |
MLNOOVGSMCJSCE-DEOSSOPVSA-N
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| InChi Code |
InChI=1S/C32H25N7O5/c1-36-27(40)17-44-21-11-9-19(10-12-21)28-22(15-33)29-37-25-7-2-3-8-26(25)39(29)30(23(28)16-34)38-31(41)20-6-4-5-18(13-20)14-24(35)32(42)43/h2-13,24H,14,17,35H2,1H3,(H,36,40)(H,38,41)(H,42,43)/t24-/m0/s1
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| Chemical Name |
(S)-2-amino-3-(3-((2,4-dicyano-3-(4-(2-(methylamino)-2-oxoethoxy)phenyl)benzo[4,5]imidazo[1,2-a]pyridin-1-yl)carbamoyl)phenyl)propanoic acid
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| Synonyms |
KMH-233 KMH 233 KMH233.
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~170.19 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.25 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 25.0 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: 2.5 mg/mL (4.25 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7019 mL | 8.5095 mL | 17.0190 mL | |
| 5 mM | 0.3404 mL | 1.7019 mL | 3.4038 mL | |
| 10 mM | 0.1702 mL | 0.8509 mL | 1.7019 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.
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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