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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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Purity: ≥98%
CBR-5884 is a novel, potent, and selective inhibitor of phosphoglycerate dehydrogenase (PHGDH) with an IC50 of 33 μM and with anticancer activities. CBR-5884 inhibits de novo serine synthesis in cancer cells and is selectively toxic to cancer cell lines with high serine biosynthetic activity. CBR-5884 selectively inhibits the proliferation of melanoma and breast cancer lines that have a high propensity for serine synthesis. Biochemical characterization of the inhibitor revealed that it was a noncompetitive inhibitor that showed a time-dependent onset of inhibition and disrupted the oligomerization state of PHGDH.
ln Vitro |
CBR-5884 (15 or 30 μM; 3-5 days) specifically prevents breast cancer and melanoma cell lines that have a strong propensity for serine synthesis from proliferating.
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Cell Assay |
Cell Proliferation Assay[1]
Cell Types: Breast cancer and melanoma cell lines Tested Concentrations: 15 or 30 μM Incubation Duration: 3-5 days Experimental Results: Inhibited proliferation of melanoma and breast cancer cell lines. |
References |
[1]. Edouard Mullarky et al. Identification of a small molecule inhibitor of 3-phosphoglycerate dehydrogenase to target serine biosynthesis in cancers Proc Natl Acad Sci U S A, 2016 Feb 16, 113(7):1778-83.
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Molecular Formula |
C14H12N2O4S2
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Molecular Weight |
336.386
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CAS # |
681159-27-3
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SMILES |
O=C(C1=CC=CO1)NC2=C(SC#N)C(C)=C(C(OCC)=O)S2
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InChi Key |
QBVIRPJBDIZKBC-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C14H12N2O4S2/c1-3-19-14(18)11-8(2)10(21-7-15)13(22-11)16-12(17)9-5-4-6-20-9/h4-6H,3H2,1-2H3,(H,16,17)
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Chemical Name |
ethyl 5-(furan-2-carboxamido)-3-methyl-4-thiocyanatothiophene-2-carboxylate
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Synonyms |
CBR-5884; CBR 5884; CBR5884.
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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 mg/mL (~148.64 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.18 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 | 2.9727 mL | 14.8637 mL | 29.7274 mL | |
5 mM | 0.5945 mL | 2.9727 mL | 5.9455 mL | |
10 mM | 0.2973 mL | 1.4864 mL | 2.9727 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.
Activity of PHGDH CBR-5884 in cells.Proc Natl Acad Sci U S A.2016 Feb 16;113(7):1778-83. th> |
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CBR-5884 inhibits serine synthesis in cells.Proc Natl Acad Sci U S A.2016 Feb 16;113(7):1778-83. td> |
CBR-5884 selectively inhibits the proliferation of breast cancer lines with a high propensity for serine synthesis.Proc Natl Acad Sci U S A.2016 Feb 16;113(7):1778-83. td> |