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Merck

SML3358

Sigma-Aldrich

AS602801

≥98% (HPLC)

Synonym(e):

1,3-Benzothiazol-2-yl(2-{[4-(morpholin-4-ylmethyl)benzyl]oxy}pyrimidin-4-yl)-acetonitrile, 2-(Benzo[d]thiazol-2-yl)-2-(2-(4-(morpholinomethyl)benzyloxy)pyrimidin-4-yl)acetonitrile, AS 602801, AS-602801, Bentamapimod, PGL 5001, PGL-5001, PGL5001

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About This Item

Empirische Formel (Hill-System):
C25H23N5O2S
CAS-Nummer:
Molekulargewicht:
457.55
MDL-Nummer:
UNSPSC-Code:
12352200
NACRES:
NA.77

Qualitätsniveau

Assay

≥98% (HPLC)

Form

powder

Farbe

white to beige

Löslichkeit

DMSO: 2 mg/mL, clear (Warmed)

Lagertemp.

2-8°C

InChI

1S/C25H23N5O2S/c26-15-20(24-28-22-3-1-2-4-23(22)33-24)21-9-10-27-25(29-21)32-17-19-7-5-18(6-8-19)16-30-11-13-31-14-12-30/h1-10,20H,11-14,16-17H2

InChIKey

XCPPIJCBCWUBNT-UHFFFAOYSA-N

Biochem./physiol. Wirkung

AS602801 (Bentamapimod, PGL5001) is an orally active, ATP-competitive, potent and selective c-Jun N-terminal kinase (JNK) inhibitor (JNK1/2/3 IC50 = 80/90/230 nM). AS602801 decreases MMP-3 upregulation in endometrium cultures from patients with endometriosis (15 μM alone or 5 μM in combination with 100-250 μM medroxyprogesterone acetate) and exhibits therapeutic efficacy in rodent endometriosis models in vivo (10-30 mg/kg via daily p.o. in mice and 10-60 mg/kg via twice daily p.o. in rats).

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable


Analysenzertifikate (COA)

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Die Dokumentenbibliothek aufrufen

Stephen S Palmer et al.
Reproductive sciences (Thousand Oaks, Calif.), 23(1), 11-23 (2015-09-04)
Endometriosis is an estrogen (ER)-dependent gynecological disease caused by the growth of endometrial tissue at extrauterine sites. Current endocrine therapies address the estrogenic aspect of disease and offer some relief from pain but are associated with significant side effects. Immune
Masahiro Yamamoto et al.
Anticancer research, 39(2), 609-617 (2019-02-04)
AS602801, an anti-cancer stem cell (CSC) candidate drug, sensitizes ovarian CSCs to paclitaxel and carboplatin by reducing the expression of survivin, an anti-apoptotic protein. The aim of the study was to examine the effect of AS602801 on the expression of
Masahiro Yamamoto et al.
Anticancer research, 38(12), 6699-6706 (2018-12-07)
AS602801, a novel inhibitor of c-Jun N-terminal kinase (JNK), suppresses tumor initiation capacity and metastatic potential of cancer stem cells (CSCs). However, it remains unknown whether this inhibitor can chemosensitize CSCs. Using A2780 CSLC, a CSC line derived from ovarian
Shuai Zhang et al.
Journal of cellular and molecular medicine, 25(8), 4062-4072 (2021-02-21)
Previous studies showed that the chemotherapeutic effect of temozolomide (TMZ) and vincristine (VCR) against glioma might be blunted by the co-culture with astrocytes, and connexin-43 (CX43) was thought to play a vital role in the communication between glioma cells and
Maohua Chen et al.
Oncotarget, 7(45), 73903-73911 (2016-09-23)
Notch signaling is a highly conserved pathway that regulates cell fate decisions during embryonic development. Notch activation endangers neurons by modulating NF-κB and HIF-1α pathways, however, the role of Notch signaling in activating JNK/c-Jun following intracerebral hemorrhage (ICH) has not

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