ChemicalBook > CAS DataBase List > Dot1L-IN-4
Dot1L-IN-4
- Product Name
- Dot1L-IN-4
- CAS No.
- 2565705-02-2
- Chemical Name
- Dot1L-IN-4
- Synonyms
- Dot1L- IN-4;QQN05022(Dot1L-IN-4);H3K79,Histone Methyltransferase,histone,methyltransferase,lysine,DOT1L,Dot1L IN 4,Inhibitor,Dot-1L-IN-4,Dot1LIN4,inhibit;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;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)-
- CBNumber
- CB78364259
- Molecular Formula
- C28H27ClF2N8O5S
- Formula Weight
- 661.08
- MOL File
- 2565705-02-2.mol
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Dot1L-IN-4 Property
- 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)
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N-Bromosuccinimide Price
ChemScene
- Product number
- CS-0109501
- Product name
- Dot1L-IN-4
- Purity
- 99.60%
- Packaging
- 5mg
- Price
- $580
- Updated
- 2021/12/16
ChemScene
- Product number
- CS-0109501
- Product name
- Dot1L-IN-4
- Purity
- 99.60%
- Packaging
- 10mg
- Price
- $980
- Updated
- 2021/12/16
ChemScene
- Product number
- CS-0109501
- Product name
- Dot1L-IN-4
- Purity
- 99.60%
- Packaging
- 25mg
- Price
- $1900
- Updated
- 2021/12/16
ChemScene
- Product number
- CS-0109501
- Product name
- Dot1L-IN-4
- Purity
- 99.60%
- Packaging
- 50mg
- Price
- $3200
- Updated
- 2021/12/16
ChemScene
- Product number
- CS-0109501
- Product name
- Dot1L-IN-4
- Purity
- 99.60%
- Packaging
- 100mg
- Price
- $5000
- Updated
- 2021/12/16
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Dot1L-IN-4 Chemical Properties,Usage,Production
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
Raw materials
Preparation Products
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