Description
Dot1L-IN-4 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 SPA DOT1L of 0.11 nM.
Product information
CAS Number: 2565705-02-2
Molecular Weight: 661.08
Formula: C28H27ClF2N8O5S
Chemical Name: 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
Smiles: COC1=NC(=NC(NC2=CC(=CC=C2N[C@@H](C2=CC=CC3OC(F)(F)OC=32)C2=NC=CC=C2Cl)S(C)(=O)=O)=N1)N1CCNCC1
InChiKey: QJIMSJUUARCROQ-QFIPXVFZSA-N
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
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 250 mg/mL (378.17 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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 (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.
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.
Products are for research use only. Not for human use.
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