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Purity: ≥98%
GLS-IN-968 is an allosteric inhibitor of glutaminase (GLS). It inhibits the transformation of fibroblasts that is dependent on Rho-GTPase and inhibits the growth and invasive activity of breast cancer cells in vitro.
Targets |
Glutaminase C
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ln Vitro |
The cellular transformation of NIH 3T3 cells is inhibited by glutaminase C-IN-1 (Compound 968; 10 μM; 14 days) [1]. Targets specific to Dbl have their signaling activity inhibited by glutaminase C-IN-1 (10 μM; 6 d) [1]. Human breast cancer cells' transforming activity is burst by glutaminase C-IN-1 [1]. In transformed cells, glutamine reset is burst by glutaminase C-IN-1 (10 μM) [2].
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Cell Assay |
Cell Viability Assay[1]
Cell Types: MDA-MB231 cells, SKBR3 cells, and NIH 3T3 cells Tested Concentrations: 10 μM Incubation Duration: 5 h Experimental Results: Inhibited -1 preferentially binds to glutaminase C in the framework state[2]. Cell growth. |
Animal Protocol |
Animal/Disease Models: P493 B lymphoma cells SCID (severe combined immunodeficient) mouse[1] Glutaminase C-IN-1 (compound 968) (200 μg/mouse; intraperitoneal (ip) injection; one time/day for 12 days) reduces tumor volume in mice[1] .
Doses: 200 μg/mouse Route of Administration: intraperitoneal (ip) injection, one time/day for 12 days Experimental Results: The tumor size was diminished by approximately 50%. |
References |
[1]. Wang JB, et al. Targeting mitochondrial glutaminase activity inhibits oncogenic transformation. Cancer Cell. 2010 Sep 14;18(3):207-19.
[2]. Stalnecker CA, et al. Mechanism by which a recently discovered allosteric inhibitor blocks glutamine metabolism in transformed cells. Proc Natl Acad Sci U S A. 2015 Jan 13;112(2):394-9. |
Molecular Formula |
C27H27BRN2O
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Molecular Weight |
475.43
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Exact Mass |
474.1307
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Elemental Analysis |
C, 68.21; H, 5.72; Br, 16.81; N, 5.89; O, 3.37
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CAS # |
311795-38-7
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Related CAS # |
311795-38-7
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Appearance |
Solid powder
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SMILES |
CC1(CC2=C(C(NC3=C2C4=CC=CC=C4C=C3)C5=CC(=C(C=C5)N(C)C)Br)C(=O)C1)C
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InChi Key |
NVFRRJQWRZFDLM-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C27H27BrN2O/c1-27(2)14-19-24-18-8-6-5-7-16(18)9-11-21(24)29-26(25(19)23(31)15-27)17-10-12-22(30(3)4)20(28)13-17/h5-13,26,29H,14-15H2,1-4H3
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Chemical Name |
5-[3-bromo-4-(dimethylamino)phenyl]-2,2-dimethyl-1,3,5,6-tetrahydrobenzo[a]phenanthridin-4-one
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Synonyms |
GLS-IN-968; GLSIN968; GLS IN 968; Glutaminase inhibitor-968; Glutaminase inhibitor compound 968; Glutaminase inhibitor 968; GLS inhibitor 968
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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 : ~25 mg/mL (~52.59 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.26 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.26 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 25.0 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 | 2.1034 mL | 10.5168 mL | 21.0336 mL | |
5 mM | 0.4207 mL | 2.1034 mL | 4.2067 mL | |
10 mM | 0.2103 mL | 1.0517 mL | 2.1034 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.
Glutaminase serves as a target for 968. Cancer Cell . 2010 Sep 14;18(3):207-19. td> |
Role of glutaminase activity in cellular transformation. Cancer Cell . 2010 Sep 14;18(3):207-19. td> |