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Merck

SML3568

C26-A6

≥98% (HPLC)

Synonym(s):

5-chloro-2-methoxy-N-(2-methyl-[1,2,4]triazolo[1,5-a]pyridin-8-yl)benzenesulfonamide

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About This Item

Empirical Formula (Hill Notation):
C14H13ClN4O3S
CAS Number:
Molecular Weight:
352.80
UNSPSC Code:
12352200
NACRES:
NA.21
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
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Quality Level

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear (Warmed)

storage temp.

2-8°C

SMILES string

O=S(NC1=CC=CN2N=C(C)N=C12)(C3=CC(Cl)=CC=C3OC)=O

InChI key

HLRMNXITZQAUIH-UHFFFAOYSA-N

Biochem/physiol Actions

A26-A6 is a MTDH-SND1 interaction blocker (IC50 = 2.4 μM by cell-free & 12.3 μM by cellular split-luc assay) that competes against metadherin (MTDH; AEG-1; LYRIC) for staphylococcal nuclease domain-containing 1 (SND1) binding, thereby preventing MTDH-SND1 complex from suppressing antitumor T cell responses. A26-A6 inhibits PyMT tumor sphere formation in cultures (IC50 <200 μM) in a MTDH- and SND1-dependent manner and exhibits in vivo efficacy against breast tumor growth and metastasis in mice in vivo (15 mg/kg/d i.v. 5d/wk), including the murine PyMT model, and human breast cancer xenografts (PDX, HCI-001, SCP28).
Metadherin-staphylococcal nuclease domain-containing 1 (MTDH-SND1) interaction inhibitor with anti-triple-negative breast cancer (TNBC) efficacy in vivo.


Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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Minhong Shen et al.
Nature cancer, 3(1), 43-59 (2022-02-06)
Metastatic breast cancer is a leading health burden worldwide. Previous studies have shown that metadherin (MTDH) promotes breast cancer initiation, metastasis and therapy resistance; however, the therapeutic potential of targeting MTDH remains largely unexplored. Here, we used genetically modified mice
Minhong Shen et al.
Nature cancer, 3(1), 60-74 (2022-02-06)
Despite increased overall survival rates, curative options for metastatic breast cancer remain limited. We have previously shown that metadherin (MTDH) is frequently overexpressed in poor prognosis breast cancer, where it promotes metastasis and therapy resistance through its interaction with staphylococcal