EPZ5676

EPZ5676
Item number Size Datasheet Manual SDS Delivery time Quantity Price
Cay16175-1 1 mg -

6 - 10 business days*

60.00€
Cay16175-5 5 mg -

6 - 10 business days*

230.00€
Cay16175-10 10 mg -

6 - 10 business days*

373.00€
Cay16175-25 25 mg -

6 - 10 business days*

641.00€
 
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:
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!
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