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Purity: =98.22%
StemRegenin 1(abbreviated as SR1; SR-1), a purine derivative, is a potent antagonist of the aryl hydrocarbon receptor (AhR) with important biological activity. It inhibits AhR with IC50 of 127 nM in CD34+ cells. SR1 has been found to promote the ex vivo expansion of CD34+ cells. SR1 has also been found to induce the ex vivo differentiation of pDCs, BDCA1+ and BDCA3+ mDCs as well as the generation of high numbers of all these DC subsets.
| Targets |
Aryl hydrocarbon receptor/AhR (IC50 = 127 nM)
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| ln Vitro |
The aryl hydrocarbon receptor is antagonistically acted upon by StemRegenin 1 (SR1). (AhR). With an EC50 of less than 120 nM, stemregenin 1 boosts the number of CD34+ cells after 5 to 7 days. Based on these findings, it can be concluded that StemRegenin 1-induced CD34+ cell growth is mediated by direct binding and AhR inhibition (IC50=40 nM). StemRegenin 1 also reduces photoaffinity ligand (PAL) binding. StemRegenin 1 (SR1), an antagonist of the aryl hydrocarbon receptor, strongly encourages the ex vivo growth of human CD34+ cells. Treatment with stemgenin 1 reduces VentX expression levels and speeds up CD34+ cell proliferation[2].
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| ln Vivo |
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| Enzyme Assay |
AhR luciferase assay. [1]
Trypsinized HepG2 cells (2 x 106 ) were transiently transfected with 20 μg of pGodLuc6.1 using Fugene6 in Opti-MEM. The transfected cells were washed and resuspended in 20 mL of MEM supplemented with 10 fetal calf serum, and plated into 384 well plates at 50 μL/well. 24 h after transfection, cells were treated with compound for 1 h prior to the addition of TCDD (3 nM). Following 24 h of induction with TCDD, luciferase activity was measured using Bright-Glo™ Luciferase Assay System (Promega). AhR ligand binding assay. [1] Experiments were performed as described previously. |
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| Cell Assay |
Human CD34+ cells were treated with 1 μm SR1 for 1 week or mock-treated (control (Ctr)). The treated cells were then harvested for analysis of VentX mRNA expression levels. F, GFP- or GFP-VentX-transfected CD34+ cells (2 × 104) were sorted and treated with 1 μm SR1 for 1 week or mock-treated. The total cell numbers were then counted and plotted.[2]
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| Animal Protocol |
Engraftment of CD34+ cells in NSG mice. [1]
A quantity of 250,000 CB-derived CD34+ cells were cultured with control conditions (DMSO, 0.01%) or StemRegenin 1 (SR1) (0.75 μM) for 3 weeks. At this point control cultures had expanded 1080-fold and StemRegenin 1 (SR1) treated cells expanded 2024-fold relative to starting cell numbers. A quantity of 30 to 30,000 uncultured CD34+ CB-derived cells or a fraction of the final culture equivalent to 30 to 10,000 starting cells were transplanted. The cells were injected intravenously via the retro-orbital route into sub-lethally irradiated (300 rads for experiment in Fig. 2A, 200 rads for experiment if Fig. 3A-B) 6- to 10-week-old NSG mice. Engraftment was performed within 24 h after irradiation. Engraftment was monitored by flow cytometric analysis of blood obtained via retro-orbital sinus or bone marrow using anti-human CD45 and anti-mouse CD45 antibodies. The mice were sacrificed between 13-16 weeks posttransplantation; bone marrow (from both femurs and tibiae), spleen and thymus were collected for analysis. For secondary engraftment, 50% of the bone marrow from each recipient mouse was transplanted into one secondary sub-lethally irradiated NSG mouse. Fifteen weeks after transplantation, bone marrow was harvested from the secondary mice and analyzed by flow cytometry. [1] |
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| References |
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| Additional Infomation |
StemRegenin 1 is inhibitor of the aryl hydrocarbon receptor
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| Molecular Formula |
C24H23N5OS
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| Molecular Weight |
429.54
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| Exact Mass |
429.162
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| Elemental Analysis |
C, 67.11; H, 5.40; N, 16.30; O, 3.72; S, 7.46
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| CAS # |
1227633-49-9
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| Related CAS # |
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| PubChem CID |
46199207
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
622.9±65.0 °C at 760 mmHg
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| Flash Point |
330.5±34.3 °C
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| Vapour Pressure |
0.0±1.9 mmHg at 25°C
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| Index of Refraction |
1.721
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| LogP |
5.1
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
31
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| Complexity |
586
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
BGFHMYJZJZLMHW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H23N5OS/c1-15(2)29-14-26-21-23(25-12-11-16-7-9-17(30)10-8-16)27-22(28-24(21)29)19-13-31-20-6-4-3-5-18(19)20/h3-10,13-15,30H,11-12H2,1-2H3,(H,25,27,28)
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| Chemical Name |
4-[2-[[2-(1-benzothiophen-3-yl)-9-propan-2-ylpurin-6-yl]amino]ethyl]phenol
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.82 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 (5.82 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.82 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3281 mL | 11.6404 mL | 23.2807 mL | |
| 5 mM | 0.4656 mL | 2.3281 mL | 4.6561 mL | |
| 10 mM | 0.2328 mL | 1.1640 mL | 2.3281 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02765997 | Withdrawn | Drug: Larotrectinib Sulfate Procedure: Bone Scan |
Biological: Unmanipulated UCB Biological: SR-1 UCB |
Masonic Cancer Center, University of Minnesota |
April 2017 | Phase 2 |
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