Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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50mg |
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Other Sizes |
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Targets |
IC50: 247 nM (EED)[1]
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ln Vitro |
PRC2 degradation is mediated by UNC6852 [1]. Even at concentrations up to 30 μM, UNC6852 does not cause death in HeLa cells [1]. Reduced EED and EZH2 levels are the effect of UNC6852 (10 μM; 1-72 hours) [1]. UNC6852 recruits VHL to facilitate PRC2 degradation [1]. EED and EZH2 are specifically degraded by UNC6852[1]. H3K27me3 levels and DLBCL cell proliferation are decreased by UNC6852 [1].
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Cell Assay |
Cell Proliferation Assay[1]
Cell Types: DLBCL Cells Tested Concentrations: 3 μM Incubation Duration: 0 -10 days Experimental Results: demonstrated anti-proliferative effects. Western Blot Analysis[1] Cell Types: HeLa Cells Tested Concentrations: 10 μM Incubation Duration: 1 hrs (hours), 4 hrs (hours), 8 hrs (hours), 10 hrs (hours), 16 hrs (hours), 20 hrs (hours), 24 hrs (hours), 48 hrs (hours), 72 hrs (hours) Experimental Results: Resulted in a decrease in the levels of both EED and EZH2. |
References |
[1]. Potjewyd F, et al. Degradation of Polycomb Repressive Complex 2 with an EED-Targeted Bivalent Chemical Degrader. Cell Chem Biol. 2020 Jan 16;27(1):47-56.e15.
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Molecular Formula |
C43H48N10O6S
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Molecular Weight |
832.97
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Exact Mass |
832.35
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Elemental Analysis |
C, 62.00; H, 5.81; N, 16.82; O, 11.52; S, 3.85
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CAS # |
2688842-08-0
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SMILES |
O=C([C@H]1N(C([C@@H](NC(CCCNC(C2=CC=C(C3=CN=C(NCC4=CC=CO4)N5C3=NN=C5)C=C2)=O)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC6=CC=C(C7=C(C)N=CS7)C=C6
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InChi Key |
PPNNFXIBKLCMTI-WXEAQWFJSA-N
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InChi Code |
InChI=1S/C43H48N10O6S/c1-26-36(60-25-48-26)29-11-9-27(10-12-29)20-45-40(57)34-19-31(54)23-52(34)41(58)37(43(2,3)4)50-35(55)8-5-17-44-39(56)30-15-13-28(14-16-30)33-22-47-42(53-24-49-51-38(33)53)46-21-32-7-6-18-59-32/h6-7,9-16,18,22,24-25,31,34,37,54H,5,8,17,19-21,23H2,1-4H3,(H,44,56)(H,45,57)(H,46,47)(H,50,55)/t31-,34+,37-/m1/s1
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Chemical Name |
(2S,4R)-1-((S)-2-(4-(4-(5-((Furan-2-ylmethyl)amino)-[1,2,4]triazolo[4,3-c]pyrimidin-8-yl)benzamido)butanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
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Synonyms |
UNC6852; UNC-6852; UNC 6852
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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 : 100 mg/mL (120.05 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (6.00 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 50.0 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: ≥ 5 mg/mL (6.00 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 50.0 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: ≥ 5 mg/mL (6.00 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 | 1.2005 mL | 6.0026 mL | 12.0052 mL | |
5 mM | 0.2401 mL | 1.2005 mL | 2.4010 mL | |
10 mM | 0.1201 mL | 0.6003 mL | 1.2005 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.