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EPZ5676

Item № 16175
CAS № 1380288-87-8
Purity ≥98%
product image
                (CAS 1380288-87-8)
SIZE PRICE QUANTITY SUBTOTAL
CART TOTAL
     1 mg $49.00 0.00
     5 mg $147.00 0.00
     10 mg $245.00 0.00
     25 mg $490.00 0.00

Pricing updated 2019-06-26. Prices are subject to change without notice.

Description

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.1,2 EPZ5676 is a highly potent aminonucleoside inhibitor of DOT1L histone methyltransferase activity (Ki = 80 pM) that demonstrates 37,000-fold selectivity over other methyltransferases.3,4 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).3 It can selectively inhibit the proliferation of acute leukemia cell lines bearing MLL translocations (IC50s range from 3.5 nM - 1.3 µM).3 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.3

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Technical Information
Formal Name
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
CAS Number
1380288-87-8
Molecular Formula
C30H42N8O3
Formula Weight
562.7
Purity
≥98%
Formulation
A crystalline solid
λmax
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

Warning - this product is not for human or veterinary use.

Shipping & Storage
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Stability
≥ 2 years
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Additional Information

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References & Product Citations
Product Description References

1. Nguyen, A.T., He, J., Taranova, O., et al. Essential role of DOT1L in maintaining normal adult hematopoiesis Cell Research 21(9), 1370-1373 (2011).

2. Bernt, K.M., and Armstrong, S.A. A role for DOT1L in MLL-rearranged leukemias Epigenomics 3(6), 667-670 (2011).

3. Daigle, S.R., Olhava, E.J., Therkelsen, C.A., et al. Potent inhibition of DOT1L as treatment of MLL-fusion leukemia Blood 122(6), 1017-1025 (2013).

4. Basavapathruni, A., Olhava, E.J., Daigle, S.R., et al. Nonclinical pharmacokinetics and metabolism of EPZ-5676, a novel DOT1L histone methyltransferase inhibitor Biopharmaceutics & Drug Disposition 35(4), 237-252 (2014).

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