Product Name :
EEDi-5285
Description:
EEDi-5285 is an exceptionally potent and orally active embryonic ectoderm development (EED) inhibitor with an IC50 value of 0.2 nM for binds to the EED protein. EEDi-5285 has anti-cancer activity.
CAS:
2488952-40-3
Molecular Weight:
479.53
Formula:
C24H22FN5O3S
Chemical Name:
8-(6-cyclopropylpyridin-3-yl)-N-[(5-fluoro-2,3-dihydro-1-benzofuran-4-yl)methyl]-1-methanesulfonylimidazo[1,5-c]pyrimidin-5-amine
Smiles :
CS(=O)(=O)C1N=CN2C=1C(=CN=C2NCC1=C(F)C=CC2OCCC1=2)C1=CN=C(C=C1)C1CC1
InChiKey:
BMLWIABJRSYZDK-UHFFFAOYSA-N
InChi :
InChI=1S/C24H22FN5O3S/c1-34(31,32)23-22-17(15-4-6-20(26-10-15)14-2-3-14)11-27-24(30(22)13-29-23)28-12-18-16-8-9-33-21(16)7-5-19(18)25/h4-7,10-11,13-14H,2-3,8-9,12H2,1H3,(H,27,28)
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
EEDi-5285 is an exceptionally potent and orally active embryonic ectoderm development (EED) inhibitor with an IC50 value of 0.2 nM for binds to the EED protein. EEDi-5285 has anti-cancer activity.|Product information|CAS Number: 2488952-40-3|Molecular Weight: 479.53|Formula: C24H22FN5O3S|Chemical Name: 8-(6-cyclopropylpyridin-3-yl)-N-[(5-fluoro-2,3-dihydro-1-benzofuran-4-yl)methyl]-1-methanesulfonylimidazo[1,5-c]pyrimidin-5-amine|Smiles: CS(=O)(=O)C1N=CN2C=1C(=CN=C2NCC1=C(F)C=CC2OCCC1=2)C1=CN=C(C=C1)C1CC1|InChiKey: BMLWIABJRSYZDK-UHFFFAOYSA-N|InChi: InChI=1S/C24H22FN5O3S/c1-34(31,32)23-22-17(15-4-6-20(26-10-15)14-2-3-14)11-27-24(30(22)13-29-23)28-12-18-16-8-9-33-21(16)7-5-19(18)25/h4-7,10-11,13-14H,2-3,8-9,12H2,1H3,(H,27,28)|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.{{Ciprofloxacin} web|{Ciprofloxacin} Apoptosis|{Ciprofloxacin} Purity & Documentation|{Ciprofloxacin} In stock|{Ciprofloxacin} manufacturer|{Ciprofloxacin} Epigenetic Reader Domain} |Shelf Life: ≥12 months if stored properly.{{Nelfinavir} web|{Nelfinavir} Metabolic Enzyme/Protease|{Nelfinavir} Biological Activity|{Nelfinavir} In Vivo|{Nelfinavir} supplier|{Nelfinavir} Autophagy} |Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.PMID:23489613 |Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|EEDi-5285 inhibits cell growth with IC50 values of 20 pM and 0.5 nM in the Pfeiffer and KARPAS422 lymphoma cell lines, respectively, carrying an EZH2 mutation.|In Vivo:|EEDi-5285 (compound 28; 50-100 mg/kg; oral gavage; daily; for 28 days; SCID mice) treatment achieves complete and durable tumor regression in the KARPAS422 xenograft model in mice with oral administration. A single 100 mg/kg oral administration of EEDi-5285 (compound 28) effectively reduces the level of H3K27me3 at 24 h in KARPAS422 tumor tissue in mice. EEDi-5285 (compound 28) achieves a Cmax of 1.8 μM and an AUC of 6.0 h▪μg/ml with 10 mg/kg oral administration and has an oral bioavailability (F) of 75%. EEDi-5285 has a moderate volume of distribution of 1.4 L/kg and a terminal T1/2 of approximately 2 h.|Products are for research use only. Not for human use.|
