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Purity: ≥98%
| Targets |
ER-alpha36 (estrogen receptor alpha 36). SNG-1153 is a modulator of estrogen receptor ER-alpha36. ER-alpha36 is a variant of the classical estrogen receptor alpha (ER-α66) that lacks both transcriptional activation domains but retains the DNA-binding domain and partial ligand-binding domain. It is involved in rapid nongenomic estrogen signaling and has been implicated in cancer progression and drug resistance. Modulation of ER-alpha36 by SNG-1153 affects cancer cell signaling and proliferation.
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| ln Vitro |
SNG-1153 is the 2nd generation small molecule for cancer therapy from Shenogen Pharma Group. SNG-1153 has inhibitory effects on TKI-resistant CML cells.
Kinase Assay: Cell Assay: SNG-1153 is the 2nd generation small molecule for cancer therapy from Shenogen Pharma Group. SNG-1153 has inhibitory effects on TKI-resistant CML cells. In vitro, SNG-1153 has inhibitory effects on TKI-resistant chronic myeloid leukemia (CML) cells. The compound shows promising activities in various in vitro models. As an ER-alpha36 modulator, SNG-1153 affects estrogen receptor signaling pathways involved in cancer cell growth and survival. The compound's activity against TKI-resistant CML cells suggests potential for overcoming drug resistance in hematological malignancies. |
| ln Vivo |
SNG1153 shows significant inhibition at low micromolar concentrations in ER-α36 overexpressed cell lines including the one resistant to tamoxifen. SNG1153 exhibited a linear PK profile with a bioavailability of more than 55% in the rat PK study. In the in-vivo efficacy studies, 3 doses were investigated and SNG1153 showed dose-dependent inhibition. The tumor growth inhibition at high dose was 57% in the breast cancer Bcap-37 xenograft model, 65% in the endometrial cancer Ishikawa xenograft model and 52% in lung adenocarcinoma SPC-A-1 xenograft model |
| Enzyme Assay |
The receptor binding assay for SNG-1153 likely involves binding studies using ER-alpha36 protein or cells expressing the receptor. Radioligand binding or fluorescence polarization assays are performed with varying concentrations of SNG-1153 and a labeled estrogen ligand. Competitive binding curves are generated to determine binding affinity. Alternatively, cell-based reporter assays using ER-alpha36-responsive elements may be used to assess the compound's modulatory effects on ER-alpha36 transcriptional activity.
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| Cell Assay |
Cells expressing ER-alpha36 (e.g., breast cancer cells or engineered cell lines) or TKI-resistant CML cells are cultured in appropriate medium. Cells are treated with increasing concentrations of SNG-1153 (typically ranging from 0.1 to 100 μM) for 48-72 hours. Cell viability is assessed using MTT, CCK-8, or CellTiter-Glo assays. ER-alpha36 signaling is assessed by Western blotting for downstream effectors or by measuring cell proliferation and apoptosis. The compound's effects on TKI-resistant cells are compared with sensitive cells to evaluate its potential for overcoming drug resistance.
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| Animal Protocol |
In vivo studies of SNG-1153 likely involve mouse xenograft models of cancer, including TKI-resistant CML or ER-alpha36-positive tumors. Immunodeficient mice are engrafted with human tumor cells subcutaneously or intravenously. When tumors are established, SNG-1153 is administered at various doses and schedules. Tumor growth is monitored, and survival is assessed. Tumors are excised for analysis of ER-alpha36 signaling and other biomarkers to confirm target engagement.
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| ADME/Pharmacokinetics |
SNG-1153 has a molecular weight of 406.35 g/mol and a molecular formula of C₂₁H₁₇F₃O₅. Detailed pharmacokinetic parameters are not extensively published. As a small molecule, SNG-1153 is expected to be orally bioavailable. The compound is a synthetic ER-alpha36 modulator developed for cancer therapy. Pharmacokinetic studies would have been conducted to support preclinical and clinical development.
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| Toxicity/Toxicokinetics |
Detailed toxicology data for SNG-1153 are limited in publicly available sources. As a cancer therapeutic, the compound would have undergone standard preclinical safety evaluation, including in vitro cytotoxicity profiling, hERG channel assessment, and in vivo toxicology studies. The compound's mechanism of action as an ER-alpha36 modulator suggests that its toxicity profile may be related to estrogen receptor modulation.
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| References | |
| Additional Infomation |
SNG-1153 is a second-generation small molecule for cancer therapy developed by Shenogen Pharma Group. It is a modulator of estrogen receptor ER-alpha36 and has inhibitory effects on TKI-resistant CML cells. The compound shows promising activities in various in vitro and in vivo models. SNG-1153 has a molecular formula of C₂₁H₁₇F₃O₅ and a molecular weight of 406.35 g/mol. It represents a potential therapeutic option for cancers involving ER-alpha36 signaling and drug-resistant malignancies.
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| Molecular Formula |
C₂₁H₁₇F₃O₅
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| Molecular Weight |
406.35
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| Exact Mass |
406.102
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| Elemental Analysis |
C, 62.07; H, 4.22; F, 14.03; O, 19.69
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| CAS # |
1446712-19-1
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| Related CAS # |
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| PubChem CID |
71621167
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| Appearance |
Solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
550.3±50.0 °C at 760 mmHg
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| Flash Point |
286.6±30.1 °C
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| Vapour Pressure |
0.0±1.5 mmHg at 25°C
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| Index of Refraction |
1.615
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| LogP |
5.49
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
29
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| Complexity |
687
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC(C1C([H])=C([H])C(=C([H])C=1[H])C1=C(C(C2=C(C([H])=C(C(C([H])([H])/C(/[H])=C(\C([H])([H])[H])/C([H])([H])[H])=C2O1)O[H])O[H])=O)O[H])(F)F
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| InChi Key |
OXHMDMVBLQNMGP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H17F3O5/c1-10(2)3-8-13-14(25)9-15(26)16-17(27)18(28)19(29-20(13)16)11-4-6-12(7-5-11)21(22,23)24/h3-7,9,25-26,28H,8H2,1-2H3
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| Chemical Name |
3,5,7-trihydroxy-8-(3-methylbut-2-enyl)-2-[4-(trifluoromethyl)phenyl]chromen-4-one
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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) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4609 mL | 12.3047 mL | 24.6093 mL | |
| 5 mM | 0.4922 mL | 2.4609 mL | 4.9219 mL | |
| 10 mM | 0.2461 mL | 1.2305 mL | 2.4609 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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