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DOT1L is a non-SET domain containing methyltransferase whose function is important for the... more
Product information "EPZ5676"
DOT1L is a non-SET domain containing methyltransferase whose function is important for the transcriptional activation of certain genes, DNA damage repair, and cell cycle regulation. DOT1L is known to play an essential role in MLL-rearranged leukemias, and thus has emerged as a drug target for these leukemias. EPZ5676 is a highly potent aminonucleoside inhibitor of DOT1L histone methyltransferase activity (Ki = 80 pM) that demonstrates 37,000-fold selectivity over other methyltransferases. In various human leukemia cell lines, EPZ5676 has been shown to inhibit the methylation of lysine 79 on histone 3 (IC50s = 3-5 nM), decreasing MLL-fusion target gene expression (IC50s = 53-67 nM). It can selectively inhibit the proliferation of acute leukemia cell lines bearing MLL translocations (IC50s range from 3.5 nM - 1.3 µM). Continuous intravenous infusion of EPZ5676 at a dose of 35 mg/kg has been reported to cause complete and sustained tumor regression in a rat xenograft model of MLL-rearranged leukemia.Formal Name: 5'-deoxy-5'-[[cis-3-[2-[6-(1,1-dimethylethyl)-1H-benzimidazol-2-yl]ethyl]cyclobutyl](1-methylethyl)amino]-adenosine. CAS Number: 1380288-87-8. Molecular Formula: C30H42N8O3. Formula Weight: 562.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 25 mg/ml, Ethanol: 30 mg/ml, Ethanol:PBS (pH 7.2) (1:8): 0.1 mg/ml. lambdamax: 255 nm. SMILES: CC(C)N(C[C@@H]1[C@@H](O)[C@@H](O)[C@H](N2C=NC3=C2N=CN=C3N)O1)[C@@H]4C[C@H](CCC5=NC(C=CC(C(C)(C)C)=C6)=C6N5)C4. InChi Code: InChI=1S/C30H42N8O3/c1-16(2)37(13-22-25(39)26(40)29(41-22)38-15-34-24-27(31)32-14-33-28(24)38)19-10-17(11-19)6-9-23-35-20-8-7-18(30(3,4)5)12-21(20)36-23/h7-8,12,14-17,19,22,25-26,29,39-40H,6,9-11,13H2,1-5H3,(H,35,36)(H2,31,32,33)/t17-,19+,22-,25-,26-. InChi Key: LXFOLMYKSYSZQS-LURJZOHASA-N.
Keywords: | 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 |
Supplier: | Cayman Chemical |
Supplier-Nr: | 16175 |
Properties
Application: | DOT1L inhibitor |
MW: | 562.7 D |
Formula: | C30H42N8O3 |
Purity: | >98% |
Format: | Crystalline Solid |
Database Information
CAS : | 1380288-87-8| Matching products |
KEGG ID : | K11427 | Matching products |
Handling & Safety
Storage: | -20°C |
Shipping: | +20°C (International: -20°C) |
Signal Word: | Warning |
GHS Hazard Pictograms: |
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H Phrases: | H302, H315, H319, H335 |
P Phrases: | P261, P264, P270, P271, P280, P301+310, P302+352, P304+340, P305+351+338, P312, P321, P330, P332+313, P337+313, P362+364, P403+233, P405, P501 |
Caution
Our products are for laboratory research use only: Not for administration to humans!
Our products are for laboratory research use only: Not for administration to humans!
Information about the product reference will follow.
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