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SM-276001 (SM276001) is a novel and potent TLR7 agonist and an orally bioactive interferon (IFN) inducer with the ability to induce antitumor immune responses. It can induce the production oof IFNα, TNFα and IL-12p40 and reduce tumor burden in the Balb/c syngeneic Renca and CT26 models.
| ln Vitro |
SM-276001 via human TLR7 activates NF-κB in a dose-dependent manner at 1 nM–10 μM[2].
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|---|---|
| ln Vivo |
When given orally to mice at a dose of 0.1 mg/kg, SM-276001 has strong IFN-inducing activity[1]. When SM-276001 is taken orally, it induces an environment of inflammatory cytokines and chemokines and activates a variety of immune effector cells, such as T and B lymphocytes, NK, and NKT cells[2]. In the Renca renal cell cancer and CT26 colorectal models, SM-276001 (3 mg/kg PO biweekly) dramatically reduces tumor growth[2]. In Balb/c and C57BL/6J mice, -276001 (orally; 0.1, 1 or 10 mg/kg) activates a variety of spleen-resident immune effector cells. The MEC of 30 nM is not reached by the plasma concentration of SM-276001 when given at doses of 1 mg/kg or higher[2].
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| Animal Protocol |
Animal/Disease Models: C57BL/6 and B6C3F1 mice bearing Renca or CT26 tumors[2]
Doses: 3 mg/kg Route of Administration: Oral administration twice weekly for 25 days Experimental Results: Dramatically decreased disease burden in mice bearing either Renca or CT26 tumors. |
| References |
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| Molecular Formula |
C16H21N7O
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|---|---|
| Molecular Weight |
327.384241819382
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| Exact Mass |
327.18
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| CAS # |
473930-22-2
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| Related CAS # |
473930-22-2;473930-50-6 (sulfate);
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| PubChem CID |
10359083
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
1.4
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
24
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| Complexity |
435
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C1NC2C(N)=NC(NCCCC)=NC=2N1CC1C=NC(C)=CC=1
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| InChi Key |
UEIOLEMXCBOQAX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H21N7O/c1-3-4-7-18-15-21-13(17)12-14(22-15)23(16(24)20-12)9-11-6-5-10(2)19-8-11/h5-6,8H,3-4,7,9H2,1-2H3,(H,20,24)(H3,17,18,21,22)
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| Chemical Name |
6-amino-2-(butylamino)-9-((6-methylpyridin-3-yl)methyl)-9H-purin-8-ol
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| Synonyms |
SM276001 SM 276001 SM-276001.
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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 : ~125 mg/mL (~381.82 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.35 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 20.8 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: ≥ 2.08 mg/mL (6.35 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 20.8 mg/mL clear DMSO stock solution to 900 μL of 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 | 3.0546 mL | 15.2728 mL | 30.5455 mL | |
| 5 mM | 0.6109 mL | 3.0546 mL | 6.1091 mL | |
| 10 mM | 0.3055 mL | 1.5273 mL | 3.0546 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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