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Documentos

SML3358

Sigma-Aldrich

AS602801

≥98% (HPLC)

Sinônimo(s):

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

Fórmula empírica (Notação de Hill):
C25H23N5O2S
Número CAS:
Peso molecular:
457.55
Número MDL:
Código UNSPSC:
12352200
NACRES:
NA.77

Nível de qualidade

Ensaio

≥98% (HPLC)

forma

powder

cor

white to beige

solubilidade

DMSO: 2 mg/mL, clear (Warmed)

temperatura de armazenamento

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

chave InChI

XCPPIJCBCWUBNT-UHFFFAOYSA-N

Ações bioquímicas/fisiológicas

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).

Código de classe de armazenamento

11 - Combustible Solids

Classe de risco de água (WGK)

WGK 3

Ponto de fulgor (°F)

Not applicable

Ponto de fulgor (°C)

Not applicable


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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
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
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
Jonas Cicenas et al.
Cancers, 10(1) (2017-12-22)
Mitogen-activated protein kinases (MAP kinases) are a family of kinases that regulates a range of biological processes implicated in the response to growth factors like latelet-derived growth factor (PDGF), epidermal growth factor (EGF), vascular endothelial growth factor (VEGF), and stress
Kenta Kuramoto et al.
Anticancer research, 38(9), 5093-5099 (2018-09-09)
Cancer stem cells (CSCs) are associated with tumorigenesis, recurrence, and metastasis. Cell-cell communication via gap junctions (GJs) between metastatic cancer cells and astrocytes is necessary for brain metastasis. Agents targeting communication between CSCs and astrocytes are expected to suppress brain

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