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| 5mg |
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| 25mg |
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9-ING-41 is a glycogen synthase kinase-3 (GSK-3) inhibitor that induces apoptosis and cell cycle arrest at prophase by targeting centrosomes and microtubule-bound GSK-3β. 9-ING-41 has anticancer activity.
| Targets |
GSK-3β (IC50 = 0.71 μM)
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|---|---|
| ln Vitro |
9-ING-41, a clinically relevant small molecule GSK-3β inhibitor with broad spectrum pre-clinical antitumor activity, suppresses the growth of neuroblastoma cells.[1] 9-ING-41 induces apoptosis and cell cycle arrest at prophase by targeting centrosomes and microtubule-bound GSK3β.[2]
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| ln Vivo |
In a mouse model of MCL, 9-ING-41 has antitumor activity as a single agent.[2] The combination of clinically relevant doses of CPT-11 and 9-ING-41 results in a greater antitumor effect than either agent alone, according to mouse xenograft studies. [1]
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| Cell Assay |
Measurement of cell viability. Relative number of viable cancer cells is determined by measuring the optical density using CellTiter 96 Aqueous One Solution Cell Proliferation Assay kit according to the manufacturer’s instructions. GraphPad Prism 6.0 software is used to determine a GI50 value for each compound using a non-linear regression model with standard slope.
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| Animal Protocol |
6–8 week-old female athymic nude mice
70 mg/kg IP |
| References | |
| Additional Infomation |
Elraglusib is under investigation in clinical trial NCT04218071 (Actuate 1901: 9-ING-41 in Myelofibrosis).
Elraglusib is a maleimide-based, small molecule inhibitor of glycogen synthase kinase-3 (GSK-3; serine/threonine-protein kinase GSK3) with potential antineoplastic activity. Upon intravenous administration, elraglusib binds to and competitively inhibits GSK-3, which may lead to downregulation of nuclear factor kappa B (NF-kappaB) and decreased expression of NF-kappaB target genes including cyclin D1, B-cell lymphoma 2 (Bcl-2), anti-apoptotic protein XIAP, and B-cell lymphoma extra-large (Bcl-XL). This may inhibit NF-kappaB-mediated survival and chemoresistance in certain tumor types. GSK-3, a constitutively active serine/threonine kinase that plays a role in numerous pathways involved in protein synthesis, cellular proliferation, differentiation, and metabolism, is aberrantly overexpressed in certain tumor types and may promote tumor cell survival and resistance to chemotherapy and radiotherapy. |
| Molecular Formula |
C22H13FN2O5
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|---|---|
| Molecular Weight |
404.347429037094
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| Exact Mass |
404.081
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| Elemental Analysis |
C, 65.35; H, 3.24; F, 4.70; N, 6.93; O, 19.78
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| CAS # |
1034895-42-5
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| Related CAS # |
1034895-42-5
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| PubChem CID |
44582816
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| Appearance |
Pink to red solid powder
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| LogP |
3.688
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
30
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| Complexity |
802
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1C=CC2=C(C=1)C(=CO2)C1C(NC(C=1C1=CN(C)C2C=C3C(=CC1=2)OCO3)=O)=O
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| InChi Key |
FARXPFGGGGLENU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H13FN2O5/c1-25-7-13(11-5-17-18(6-15(11)25)30-9-29-17)19-20(22(27)24-21(19)26)14-8-28-16-3-2-10(23)4-12(14)16/h2-8H,9H2,1H3,(H,24,26,27)
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| Chemical Name |
3-(5-fluorobenzofuran-3-yl)-4-(5-methyl-5H-[1,3]dioxolo[4,5-f]indol-7-yl)-1H-pyrrole-2,5-dione
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| Synonyms |
9-ING-41; 9 ING 41; 9ING41
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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: 50~81 mg/mL (123.7~200.3 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.18 mM) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4731 mL | 12.3655 mL | 24.7310 mL | |
| 5 mM | 0.4946 mL | 2.4731 mL | 4.9462 mL | |
| 10 mM | 0.2473 mL | 1.2366 mL | 2.4731 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 | Status | Interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04218071 | Active Recruiting |
Drug: Ruxolitinib Drug: 9-ING-41 |
Myelofibrosis | Actuate Therapeutics Inc. | August 20, 2020 | Phase 2 |
| NCT05010629 | Recruiting | Drug: 9-ING-41 Drug: Carboplatin |
Metastatic Cancer Salivary Gland Cancer |
Glenn J. Hanna | September 14, 2021 | Phase 2 |
| NCT05077800 | Recruiting | Drug: 9-ING-41 Drug: Losartan |
Pancreatic Adenocarcinoma | Colin D. Weekes, M.D. | March 21, 2022 | Phase 2 |
| NCT03678883 | Recruiting | Drug: 9-ING-41 Drug: Doxorubicin. |
Cancer Sarcoma |
Actuate Therapeutics Inc. | January 4, 2019 | Phase 2 |
| NCT05239182 | Active Recruiting |
Drug: 9-ING-41 Drug: Abraxane |
Pancreatic Adenocarcinoma | Anwaar Saeed | January 26, 2022 | Phase 2 |
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