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Dot1L-IN-4

Product Name
Dot1L-IN-4
CAS No.
2565705-02-2
Chemical Name
Dot1L-IN-4
Synonyms
Dot1L- IN-4;Dot1L-IN-4/QQN05022;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)-;N1-[(S)-(3-chloropyridin-2-yl)(2,2-difluoro-2H-1,3-benzodioxol-4-yl)methyl]-4-methanesulfonyl-N2-[4-methoxy-6-(piperazin-1-yl)-1,3,5-triazin-2-yl]benzene-1,2-diamine;(S)-N1-((3-Chloropyridin-2-yl)(2,2-difluorobenzo[d][1,3]dioxol-4-yl)methyl)-N2-(4-methoxy-6-(piperazin-1-yl)-1,3,5-triazin-2-yl)-4-(methylsulfonyl)benzene-1,2-diamine
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)
color 
White to light yellow
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P501Dispose of contents/container to..…

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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

Uses

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].

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].

in vivo

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].

Animal Model:Male mice (C57BL/6) bearing subcutaneous MV4-11 tumor xenografts[1]
Dosage:300 mg/kg (Pharmacokinetic Analysis)
Administration:P.o.
Result:Was 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 were reduced only by less than half as compared to control animals.

IC 50

DOT1L: 0.11 nM (IC50)

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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Dot1L-IN-4 Suppliers

China 27 United States 4 Global 31
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4817
Advantage
55
Shanghai YuanYe Biotechnology Co., Ltd.
Tel
021-61312847; 18021002903
Fax
QQ:3008007432
Email
3008007409@qq.com
Country
China
ProdList
86249
Advantage
60
ShangHai Biochempartner Co.,Ltd
Tel
177-54423994 17754423994
Fax
QQ:2853530913
Email
2853530910@QQ.com
Country
China
ProdList
8000
Advantage
62
Shanghai Chaolan Chemical Technology Center
Tel
021-QQ：65489617 15618227136
Fax
21-5161 9052
Email
Sales@ATKchemical.com
Country
China
ProdList
9505
Advantage
58
Heze Development Zone chuangli Chemical Co., Ltd.
Tel
0530-+86-530-529 6766，+86-15666160102 15666160102
Fax
0530-529 6766
Email
info@chuangli-chem.com
Country
China
ProdList
840
Advantage
55
InvivoChem
Tel
+1-708-310-1919 +1-13798911105
Fax
708-557-7486
Email
sales@invivochem.cn
Country
United States
ProdList
6391
Advantage
58
Changzhou Chenhong Biotechnology Co., Ltd.
Tel
+86-0519-85788828 +86-13775037613
Email
sales@chemrenpharm.com
Country
China
ProdList
4032
Advantage
58
Chunchuang (Wuhan) Technology Co., Ltd
Tel
15727060112
Email
yutianchun2007@126.com
Country
China
ProdList
9856
Advantage
58
NewCan Biotech Limited
Tel
+86-0571-86912261 +86-15658003402
Fax
311113
Email
sales@newcanbio.com
Country
China
ProdList
1613
Advantage
58
Bide Pharmatech Ltd.
Tel
400-1647117 13681763483
Email
product02@bidepharm.com
Country
China
ProdList
59936
Advantage
58

2565705-02-2, Dot1L-IN-4Related Search:


  • 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
  • N1-[(S)-(3-chloropyridin-2-yl)(2,2-difluoro-2H-1,3-benzodioxol-4-yl)methyl]-4-methanesulfonyl-N2-[4-methoxy-6-(piperazin-1-yl)-1,3,5-triazin-2-yl]benzene-1,2-diamine
  • (S)-N1-((3-Chloropyridin-2-yl)(2,2-difluorobenzo[d][1,3]dioxol-4-yl)methyl)-N2-(4-methoxy-6-(piperazin-1-yl)-1,3,5-triazin-2-yl)-4-(methylsulfonyl)benzene-1,2-diamine
  • Dot1L-IN-4/QQN05022
  • 2565705-02-2
  • C28H27ClF2N8O5S