| Company Name: |
Wuhan Acumen Bio-Technology Co.,ltd Gold
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| Tel: |
027-027-16602739303 16602739303 |
| Email: |
673003916@qq.com |
| Products Intro: |
Product Name:Dot1L-IN-4
CAS:2565705-02-2
Purity:95%,98% Package:5G
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| | Dot1L-IN-4 Basic information |
| Product Name: | Dot1L-IN-4 | | Synonyms: | 1,2-Benzenediamine, N1-[(S)-(3-chloro-2-pyridinyl)(2,2-difluoro-1,3-benzodioxol-4-yl)methyl]-N2-[4-methoxy-6-(1-piperazinyl)-1,3,5-triazin-2-yl]-4-(methylsulfonyl)-;Dot1L- IN-4;QQN05022(Dot1L-IN-4);N1-[(3-Chloro-pyridin-2-yl)-(2,2-difluoro-benzo[1,3]dioxol-4-yl)-methyl]-4-methanesulfonyl-N2-(4-methoxy-6-piperazin-1-yl-[1,3,5]triazin-2-yl)-benzene-1,2-diamine;H3K79,Histone Methyltransferase,histone,methyltransferase,lysine,DOT1L,Dot1L IN 4,Inhibitor,Dot-1L-IN-4,Dot1LIN4,inhibit | | CAS: | 2565705-02-2 | | MF: | C28H27ClF2N8O5S | | MW: | 661.08 | | EINECS: | | | Product Categories: | | | Mol File: | 2565705-02-2.mol |  |
| | Dot1L-IN-4 Chemical Properties |
| Boiling point | 792.1±70.0 °C(Predicted) | | density | 1.58±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO : 250 mg/mL (378.17 mM; Need ultrasonic) | | form | A solid | | pka | 8.67±0.10(Predicted) | | color | White to light yellow |
| | Dot1L-IN-4 Usage And Synthesis |
| Biological Activity | Dot1L-IN-4 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 SPA DOT1L of 0.11 nM[1].
Dot1L-IN-4 (Compound 10) is tested in cellular assays to assess the ability to inhibit the dimethylation of H3K79 in HeLa cells (ED50 H3K79me2 Elisa=1.7 nM) and HOXA9 gene expression in Molm-13 cells (ED50 HOXA9 RGA=33 nM). Dot1L-IN-4 also inhibits mixed lineage leukemia (MLL) with an IC50 of 99 μM[1].
Dot1L-IN-4 (Compound 10; 300 mg/kg; p.o.; qd) is not tolerated at such a high dose by tumor xenograft bearing mice, and at a 6-fold reduced dose, the tumor growth as well as the HOXA9 reporter gene mRNA are reduced only by less than half as compared to control animals[1]. | | References | [1]. Frédéric Stauffer, et al. New Potent DOT1L Inhibitors for in Vivo Evaluation in Mouse. ACS Med. Chem. Lett. 2019, 10, 12, 1655-1660. |
| | Dot1L-IN-4 Preparation Products And Raw materials |
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