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Dot1L-IN-4 - 99%, high purity , CAS No.2565705-02-2

COA COA
    Grade & Purity:
  • ≥99%
In stock
Item Number
D648943
Grouped product items
SKU Size
Availability
 Price Qty
D648943-1mg
1mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$238.90
D648943-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$500.90
D648943-10mg
10mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$850.90
D648943-25mg
25mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$1,500.90
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View related series
Epigenetics (1496) Histone Methyltransferase (190) Histone Modification (1379)

Basic Description

Specifications & Purity ≥99%
Biochemical and Physiological Mechanisms Dot1L-IN-4 is a potent disruptor of telomeric silencing 1-like protein ( DOT1L ) inhibitor with an IC 50 SPA DOT1L of 0.11 nM.
Storage Temp Store at -20°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Product Description

Dot1L-IN-4 is a potent disruptor of telomeric silencing 1-like protein ( DOT1L ) inhibitor with an IC 50 SPA DOT1L of 0.11 nM

In Vitro

Dot1L-IN-4 (Compound 10) is tested in cellular assays to assess the ability to inhibit the dimethylation of H3K79 in HeLa cells (ED 50 H3K79me2 Elisa =1.7 nM) and HOXA9 gene expression in Molm-13 cells (ED 50 HOXA9 RGA =33 nM). Dot1L-IN-4 also inhibits mixed lineage leukemia (MLL) with an IC 50 of 99 µM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male mice (C57BL/6) bearing subcutaneous MV4-11 tumor xenografts 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.

Form:Solid

IC50& Target:DOT1L 0.11 nM (IC 50 )

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Organoheterocyclic compounds
Class Diazinanes
Subclass Piperazines
Intermediate Tree Nodes Not available
Direct Parent N-arylpiperazines
Alternative Parents Sulfonylanilines  Benzodioxoles  Benzenesulfonyl compounds  Phenylalkylamines  Dialkylarylamines  2-methoxy-1,3,5-triazines  1,3,5-triazine-2,4-diamines  Secondary alkylarylamines  Alkyl aryl ethers  Pyridines and derivatives  Aryl chlorides  Sulfones  Heteroaromatic compounds  Oxacyclic compounds  Dialkylamines  Azacyclic compounds  Organopnictogen compounds  Organofluorides  Organochlorides  Organic oxides  Hydrocarbon derivatives  Alkyl fluorides  
Molecular Framework Aromatic heteropolycyclic compounds
Substituents N-arylpiperazine - Sulfonylaniline - Benzenesulfonyl group - Benzodioxole - 2,4-diamine-s-triazine - 2-methoxy-1,3,5-triazine - Alkoxy-s-triazine - Phenylalkylamine - Aniline or substituted anilines - Dialkylarylamine - Aralkylamine - Secondary aliphatic/aromatic amine - Aminotriazine - Amino-1,3,5-triazine - Alkyl aryl ether - 1,3,5-triazine - Benzenoid - Triazine - Pyridine - Monocyclic benzene moiety - Aryl halide - Aryl chloride - Heteroaromatic compound - Sulfonyl - Sulfone - Oxacycle - Azacycle - Secondary amine - Ether - Secondary aliphatic amine - Organic nitrogen compound - Organic oxygen compound - Organopnictogen compound - Organic oxide - Hydrocarbon derivative - Organosulfur compound - Organooxygen compound - Organonitrogen compound - Organofluoride - Organochloride - Organohalogen compound - Amine - Alkyl halide - Alkyl fluoride - Aromatic heteropolycyclic compound
Description This compound belongs to the class of organic compounds known as n-arylpiperazines. These are organic compounds containing a piperazine ring where the nitrogen ring atom carries an aryl group.
External Descriptors Not available

Associated Targets(Human)

DOT1L Tchem Histone-lysine N-methyltransferase, H3 lysine-79 specific (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
MV4-11 (7307 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SETD7 Tchem Histone-lysine N-methyltransferase SETD7 (390 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
EHMT2 Tchem Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 (93046 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
DOT1L Tchem Histone-lysine N-methyltransferase, H3 lysine-79 specific (648 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
KMT5A Tchem N-lysine methyltransferase SETD8 (202 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SUV39H2 Tchem Histone-lysine N-methyltransferase SUV39H2 (524 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SMYD2 Tchem N-lysine methyltransferase SMYD2 (395 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
NSD3 Tchem Histone-lysine N-methyltransferase NSD3 (55 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SETD2 Tchem Histone-lysine N-methyltransferase SETD2 (119 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Associated Targets(non-human)

Mus musculus (284745 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Carm1 Histone-arginine methyltransferase CARM1 (53 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Mechanisms of Action

Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name References

Names and Identifiers

IUPAC Name 1-N-[(S)-(3-chloropyridin-2-yl)-(2,2-difluoro-1,3-benzodioxol-4-yl)methyl]-2-N-(4-methoxy-6-piperazin-1-yl-1,3,5-triazin-2-yl)-4-methylsulfonylbenzene-1,2-diamine
INCHI InChI=1S/C28H27ClF2N8O5S/c1-42-27-37-25(36-26(38-27)39-13-11-32-12-14-39)35-20-15-16(45(2,40)41)8-9-19(20)34-22(23-18(29)6-4-10-33-23)17-5-3-7-21-24(17)44-28(30,31)43-21/h3-10,15,22,32,34H,11-14H2,1-2H3,(H,35,36,37,38)/t22-/m0/s1
InChIKey QJIMSJUUARCROQ-QFIPXVFZSA-N
Smiles COC1=NC(=NC(=N1)N2CCNCC2)NC3=C(C=CC(=C3)S(=O)(=O)C)NC(C4=C5C(=CC=C4)OC(O5)(F)F)C6=C(C=CC=N6)Cl
Isomeric SMILES COC1=NC(=NC(=N1)N2CCNCC2)NC3=C(C=CC(=C3)S(=O)(=O)C)N[C@@H](C4=C5C(=CC=C4)OC(O5)(F)F)C6=C(C=CC=N6)Cl
PubChem CID 145704695
Molecular Weight 661.08

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Chemical and Physical Properties

Solubility DMSO : ≥ 220 mg/mL (332.79 mM)

Solution Calculators

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