Size | Price | Stock | Qty |
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5mg |
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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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500mg |
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Other Sizes |
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Purity: ≥98%
ln Vitro |
When bound to CARM1, EZM 2302 exhibits broad selectivity for other histone methyltransferases while selectively inhibiting CARM1 activity (IC50=6 nM). Applying EZM 2302 to MM cell lines prevents cell arrest and PABP1 and SMB methylation, with IC50 values in the nanomolar range (9 and 31 nM, respectively). Many hematopoietic cell lines are inhibited in vitro by EZM 2302; at day 14, the IC50 values for 9 out of 15 cell lines were less than 100 nM [1].
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ln Vivo |
EZM 2302 exhibits stability in human hepatocytes (CL<3 mL/min/kg) and exhibits moderate binding to plasma proteins in mice, rats, and humans, with average unbound fractions of 0.66, 0.46, and 0.74, in that order. The plasma clearance (CL) in rats and mice was 91 mL/min/kg and 43 mL/min/kg, respectively. Following 21 days in the RPMI-8226 xenograft model, EZM 2302 showed dose-dependent exposure and tumor growth inhibition (TGI). On day 21, tumor development in all EZM 2302 dosing groups was significantly slower than that of the vehicle [1].
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References |
[1]. Drew AE, et al. Identification of a CARM1 Inhibitor with Potent In Vitro and In Vivo Activity in Preclinical Models of Multiple Myeloma. Sci Rep. 2017 Dec 21;7(1):17993
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Molecular Formula |
C29H37CLN6O5
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Molecular Weight |
585.1
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Exact Mass |
584.2514
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CAS # |
1628830-21-6
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SMILES |
O=C(N(CC1)CCC21CN(C3=NC(C4=CC(OC[C@H](O)CNC)=CC=C4Cl)=NC(C5=C(C)ON=C5C)=C3C)C2)OC
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InChi Key |
OWCOTUVKROVONT-HXUWFJFHSA-N
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InChi Code |
InChI=1S/C29H37ClN6O5/c1-17-25(24-18(2)34-41-19(24)3)32-26(22-12-21(6-7-23(22)30)40-14-20(37)13-31-4)33-27(17)36-15-29(16-36)8-10-35(11-9-29)28(38)39-5/h6-7,12,20,31,37H,8-11,13-16H2,1-5H3/t20-/m1/s1
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Chemical Name |
Methyl (R)-2-(2-(2-chloro-5-(2-hydroxy-3-(methylamino)propoxy)phenyl)-6-(3,5-dimethylisoxazol-4-yl)-5-methylpyrimidin-4-yl)-2,7-diazaspiro[3.5]nonane-7-carboxylate
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Synonyms |
EZM2302 GSK3359088EZM-2302 GSK-3359088EZM 2302 GSK 3359088
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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 (~170.91 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.27 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. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.56 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 20.8 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.56 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. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.7091 mL | 8.5455 mL | 17.0911 mL | |
5 mM | 0.3418 mL | 1.7091 mL | 3.4182 mL | |
10 mM | 0.1709 mL | 0.8546 mL | 1.7091 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.