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| Targets |
SR13800 is a potent inhibitor of monocarboxylate transporter 1 (MCT1), a transporter involved in the uptake of lactate and other monocarboxylates. By inhibiting MCT1, SR13800 blocks lactate uptake and metabolism in cancer cells, leading to reduced proliferation and survival. Its mechanism involves inhibition of MCT1-mediated transport. SR13800 has anti-cancer activity and is cell-permeable.
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| ln Vitro |
MCT1-IN-2 (compound 3) exhibits a pKi of 9.48 for Jurkat T cells and a pIC50 of 8.61 for human peripheral blood mononuclear cells (PBMC) [1]. When it comes to human Raji lymphoma cell proliferation, MCT1-IN-2 (Compound 1) exhibits an EC50 of 5.5 nM (MTT assay) and an IC50 of 105 nM (lactate transport inhibition assay) [2].
In vitro, SR13800 is a potent MCT1 inhibitor with an IC50 of 0.5 nM. It blocks proliferation of Raji lymphoma cells in vitro and inhibits lactate uptake in breast cancer cells in vitro. Its in vitro activity is characterized by potent inhibition of MCT1 and antiproliferative effects on cancer cells. SR13800 has anti-cancer activity. |
| ln Vivo |
In vivo, SR13800 has potential anti-cancer activity. As an MCT1 inhibitor, it may block lactate uptake and metabolism in tumors, leading to reduced tumor growth. However, detailed in vivo efficacy data for specific disease models are limited. SR13800 is primarily used as a research tool for studying MCT1 biology and cancer metabolism.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for SR13800 are not typical, as it acts by inhibiting MCT1 transport rather than binding to a specific enzyme. However, its inhibition of MCT1-mediated lactate uptake can be measured using transport assays. These assays confirm its mechanism of action as an MCT1 inhibitor.
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| Cell Assay |
In vitro cellular assays for SR13800 typically involve treating cancer cell lines such as Raji lymphoma cells and breast cancer cells with the compound and measuring cell proliferation and lactate uptake. SR13800 blocks proliferation of Raji lymphoma cells and inhibits lactate uptake in breast cancer cells in vitro. These cell-based studies demonstrate its functional inhibition of MCT1 and its antiproliferative effects.
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| Animal Protocol |
In vivo animal models for SR13800 may include xenograft tumor models to evaluate its anti-cancer efficacy. The compound is administered by appropriate routes, and tumor growth inhibition is measured. However, detailed animal protocol information is limited. SR13800 is primarily used as a research tool for studying MCT1 biology and cancer metabolism.
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| ADME/Pharmacokinetics |
SR13800 has a molecular weight of 435.58 and a molecular formula of C25H29N3O2S. Its CAS number is 227321-12-2. The compound is also known as MCT1-IN-2. It is a potent, cell-permeable inhibitor of monocarboxylate transporter 1 (MCT1) with an IC50 of 0.5 nM. SR13800 has anti-cancer activity.
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| Toxicity/Toxicokinetics |
SR13800 is an MCT1 inhibitor with a well-characterized mechanism of action. As with any transporter inhibitor, potential toxicity may include effects on lactate metabolism and pH homeostasis. The compound's safety profile should be evaluated in preclinical toxicology studies. SR13800 is for research use only and is not approved for human therapeutic use. It represents a valuable tool for studying MCT1 biology and cancer metabolism.
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| References | |
| Additional Infomation |
SR13800 (CAS# 227321-12-2) is a potent, cell-permeable inhibitor of monocarboxylate transporter 1 (MCT1) with an IC50 of 0.5 nM. It blocks proliferation of Raji lymphoma cells and inhibits lactate uptake in breast cancer cells in vitro. SR13800 has anti-cancer activity. The compound is for research use only and not for human therapeutic use.
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| Molecular Formula |
C25H29N3O2S
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| Molecular Weight |
435.581664800644
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| Exact Mass |
435.198
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| CAS # |
227321-12-2
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| PubChem CID |
5282542
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| Appearance |
White to off-white solid powder
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| LogP |
4.6
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
31
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| Complexity |
655
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(CCCO)C1=C2C(N(C)N=C(CC(C)C)C2=CN1CC1=CC=CC2C=CC=CC1=2)=O
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| InChi Key |
VDAVMXLEMHVXOG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H29N3O2S/c1-17(2)14-22-21-16-28(15-19-10-6-9-18-8-4-5-11-20(18)19)25(31-13-7-12-29)23(21)24(30)27(3)26-22/h4-6,8-11,16-17,29H,7,12-15H2,1-3H3
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| Chemical Name |
5-(3-hydroxypropylsulfanyl)-3-methyl-1-(2-methylpropyl)-6-(naphthalen-1-ylmethyl)pyrrolo[3,4-d]pyridazin-4-one
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| Synonyms |
SR 13800 SR-13800 SR13800
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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 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)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~229.6 mM; with ultrasonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.74 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 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 DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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 (5.74 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 DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2958 mL | 11.4789 mL | 22.9579 mL | |
| 5 mM | 0.4592 mL | 2.2958 mL | 4.5916 mL | |
| 10 mM | 0.2296 mL | 1.1479 mL | 2.2958 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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