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

  • ≥99%
Item Number
D648943
Grouped product items
SKUSizeAvailabilityPrice 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
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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

Basic Description

Specifications & Purity≥99%
Biochemical and Physiological MechanismsDot1L-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 TempStore at -20°C
Shipped InIce chest + Ice pads
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 )

Associated Targets(Human)

DOT1L Tchem Histone-lysine N-methyltransferase, H3 lysine-79 specific (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MV4-11 (7307 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SETD7 Tchem Histone-lysine N-methyltransferase SETD7 (390 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
EHMT2 Tchem Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 (93046 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
DOT1L Tchem Histone-lysine N-methyltransferase, H3 lysine-79 specific (648 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
KMT5A Tchem N-lysine methyltransferase SETD8 (202 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SUV39H2 Tchem Histone-lysine N-methyltransferase SUV39H2 (524 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SMYD2 Tchem N-lysine methyltransferase SMYD2 (395 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NSD3 Tchem Histone-lysine N-methyltransferase NSD3 (55 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SETD2 Tchem Histone-lysine N-methyltransferase SETD2 (119 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
WDR5 Tchem MLL1/ASH2L/RBBP5/WDR5 complex (16 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Mus musculus (284745 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Carm1 Histone-arginine methyltransferase CARM1 (53 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

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
InChi Key QJIMSJUUARCROQ-QFIPXVFZSA-N
Canonical 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

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Chemical and Physical Properties

SolubilityDMSO : ≥ 220 mg/mL (332.79 mM)

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