Dot1L-IN-5 - ≥98% , CAS No.2565705-03-3

CAS: 2565705-03-3 Cat. No.: D646409 분자식: C₂₃H₁₉ClF₂N₈O₅S 분자량: 592.96

GRADE & PURITY ≥98%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

개요

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.

Form:Solid

IC50& Target:DOT1L 0.17 nM (IC 50 )

Specifications

사양 및 순도

≥98%

생화학 및 생리적 메커니즘

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

보관 조건

Store at -20°C

배송

Ice chest + Ice pads

이 제품은 콜드 체인 배송이 필요합니다.지상 및 기타 경제 서비스는 사용할 수 없습니다.

작업 유형

INHIBITOR

순수함

≥98%

이름과 식별자

• 분자량: 592.96

화학 및 물리적 특성

• 용해성: DMSO : 250 mg/mL (421.61 mM; Need ultrasonic)