- Pinometostat
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- $81.00
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2026-07-31
- CAS:1380288-87-8
- Purity: 99.97%
- Supply Ability: 10g
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| | (2R,3R,4S,5R)-2-(6-aMino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]iMidazol-2-yl)ethyl)cyclobutyl)(isopropyl)aMino)Methyl)tetrahydrofuran-3,4-diol Basic information |
| Product Name: | (2R,3R,4S,5R)-2-(6-aMino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]iMidazol-2-yl)ethyl)cyclobutyl)(isopropyl)aMino)Methyl)tetrahydrofuran-3,4-diol | | Synonyms: | (2R,3R,4S,5R)-2-(6-aMino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]iMidazol-2-yl)ethyl)cyclobutyl)(isopropyl)aMino)Methyl)tetrahydrofuran-3,4-diol;EPZ 5676;9-[5-Deoxy-5-[[cis-3-[2-[6-(1,1-diMethylethyl)-1H-benziMidazol-2-yl]ethyl]cyclobutyl](1-Methylethyl)aMino]-β-D-ribofuranosyl]-9H-purin-6-aMine;9-[5-Deoxy-5-[[cis-3-[2-[6-(1,1-dimethylethyl)-1H-benzimidazol-2-yl]ethyl]cyclobutyl](1-methylethyl)amino]-beta-D-ribofuranosyl]-9H-purin-6-amine;9H-Purin-6-amine, 9-[5-deoxy-5-[[cis-3-[2-[6-(1,1-dimethylethyl)-1H-benzimidazol-2-yl]ethyl]cyclobutyl](1-methylethyl)amino]-β-D-ribofuranosyl]-;9-[5-Deoxy-5-[[cis-3-[2-[6-(1,1-diMethylethyl)-1H-benziMidazol-2-yl]ethyl]cyclobutyl](1-Methylethyl)aMino]-β-D-ribofuranosyl]-9H-purin-6-aMine EPZ-5676;EPZ5676, >=98%;EPZ-5676,Pinometostat | | CAS: | 1380288-87-8 | | MF: | C30H42N8O3 | | MW: | 562.71 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 1380288-87-8.mol | ![(2R,3R,4S,5R)-2-(6-aMino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]iMidazol-2-yl)ethyl)cyclobutyl)(isopropyl)aMino)Methyl)tetrahydrofuran-3,4-diol Structure](CAS/20150408/GIF/1380288-87-8.gif) |
| | (2R,3R,4S,5R)-2-(6-aMino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]iMidazol-2-yl)ethyl)cyclobutyl)(isopropyl)aMino)Methyl)tetrahydrofuran-3,4-diol Chemical Properties |
| Boiling point | 835.3±75.0 °C(Predicted) | | density | 1.45±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | ≥28.15 mg/mL in DMSO; insoluble in H2O; ≥50.3 mg/mL in EtOH with ultrasonic | | form | solid | | pka | 12.34±0.10(Predicted) | | color | White to light yellow |
| | (2R,3R,4S,5R)-2-(6-aMino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]iMidazol-2-yl)ethyl)cyclobutyl)(isopropyl)aMino)Methyl)tetrahydrofuran-3,4-diol Usage And Synthesis |
| Uses | 9-[5-Deoxy-5-[[cis-3-[2-[6-(1,1-dimethylethyl)-1H-benzimidazol-2-yl]ethyl]cyclobutyl](1-methylethyl)amino]-β-D-ribofuranosyl]-9H-purin-6-amine, can be used as an adenosine anticancer, and antibiotic analogues. | | Definition | ChEBI: (2R,3R,4S,5R)-2-(6-aminopurin-9-yl)-5-[[[3-[2-(6-tert-butyl-1H-benzimidazol-2-yl)ethyl]cyclobutyl]-propan-2-ylamino]methyl]oxolane-3,4-diol is a 5'-deoxyribonucleoside. | | Biological Activity | epz5676 is a potent inhibitor of dot1l histone methyltransferase, according to x-ray crystallographic analysis, that occupies the s-adenosyl methionine (sam) binding pocket of dot1l and induces conformational changes in dot1l resulting in the opening of a hydrophobic pocket beyond the amino acid portion of sam. epz5676 selectively inhibits dotil with a value of 50% inhibition concentration ic50 of 0.8 nm, which is 37000-fold greater in selectivity than other methyltransferases, including carm1, ehmt1/2, ezh1/2, prmt1/2/5/6/8, setd7, smyd2/3, and whsc1/1l1. epz5676 has been investigated for the treatment of mll-rearranged leukemia in multiple studies where results have shown that epz5676 inhibits h3k79 methylation and the expression of mll-fusion target gene and potently kills acute leukemia cell lines bearing mll translocation.daigle sr, olhava ej, therkelsen ca, basavapathruni a, jin l, boriack-sjodin pa, allain cj, klaus cr, raimondi a, scott mp, waters nj, chesworth r, moyer mp, copeland ra, richon vm, pollock rm. potent inhibition of dot1l as treatment of mll-fusion leukemia. blood. 2013 aug 8;122(6):1017-1025. | | in vivo | Pinometostat (EPZ-5676) (70 mg/kg, i.p.) causes complete and sustained regression in a rat xenograft model of MLL-rearranged leukemia. Pinometostat (EPZ-5676) (70, 35 mg/kg, i.v.) reduces HOXA9 and MEIS1 mRNA levels of tumors taken from rats, and reduces MLL-fusion target gene expression in vivo[1]. | | target | DOT1L | | IC 50 | DOT1L |
| | (2R,3R,4S,5R)-2-(6-aMino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]iMidazol-2-yl)ethyl)cyclobutyl)(isopropyl)aMino)Methyl)tetrahydrofuran-3,4-diol Preparation Products And Raw materials |
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