Dot1L-IN-5 - 10mM in DMSO , CAS No.2565705-03-3

CAS: 2565705-03-3 Cat. No.: D654571 Molecular Weight: 592.96

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Dot1L-IN-5 is a potent disruptor of telomeric silencing 1-like protein ( DOT1L ) inhibitor with an IC 50 of 0.17 nM

In Vitro

Dot1L-IN-5 (Compound 11) is tested in cellular assays to assess the ability to inhibit the dimethylation of H3K79 in HeLa cells (ED 50 H3K79me2 Elisa =2.9 nM) and HOXA9 gene expression in Molm-13 cells (ED 50 HOXA9 RGA =30 nM). MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Dot1L-IN-5 (Compound 11; subcutaneous injection; at 75 mg/kg once daily for 20 days) does not lead to tumor growth inhibition in NOD-SCID mice. Dot1L-IN-5 (subcutaneous injection; at 75 mg/kg twice daily for 20 days) leads 73% growth inhibition . While both treatment regimens result in very strong inhibition of global H3K79 dimethylation level in tumor, the efficacious regimen is superior in reducing the mRNA expression of the target genes HOXA9 and MEIS1 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: NOD-SCID mice bearing subcutaneous MV4-11 tumor xenografts Dosage: 75 mg/kg Administration: Subcutaneous injection; at 75 mg/kg once or twice daily for 20 days Result: Once daily administration did not lead to tumor growth inhibition, 73% growth inhibition was measured in the twice daily treated group.

IC50& Target:DOT1L 0.17 nM (IC 50 )

Specifications

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

Dot1L-IN-5 is a potent disruptor of telomeric silencing 1-like protein ( DOT1L ) inhibitor with an IC 50 of 0.17 nM.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

INHIBITOR

Names and Identifiers

• Molecular Weight: 592.96