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Merck

573097

WP1066

≥97% (HPLC), STAT3 pathway inhibitor, solid

Synonyme(s) :

STAT3 Inhibitor III, WP1066

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A propos de cet article

Formule empirique (notation de Hill) :
C17H14BrN3O
Numéro CAS:
857064-38-1
Poids moléculaire :
356.22
MDL number:
MFCD12912450
UNSPSC Code:
12352200
NACRES:
NA.77

Principaux documents

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Nom du produit

STAT3 Inhibitor III, WP1066, STAT3 Inhibitor III, WP1066, CAS 857064-38-1, is a cell-permeable AG490 tyrphostin analog that acts as a STAT3 pathway inhibitor. A potent anti-tumor agent.

SMILES string

Brc1nc(ccc1)\C=C(\C(=O)N[C@@H](C)c2ccccc2)/C#N

InChI

1S/C17H14BrN3O/c1-12(13-6-3-2-4-7-13)20-17(22)14(11-19)10-15-8-5-9-16(18)21-15/h2-10,12H,1H3,(H,20,22)/b14-10+/t12-/m0/s1

InChI key

VFUAJMPDXIRPKO-LQELWAHVSA-N

assay

≥97% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

off-white

solubility

DMSO: 10 mg/mL
ethanol: 5 mg/mL

shipped in

ambient

storage temp.

2-8°C

Quality Level

100

Catégories apparentées

Biochem/physiol Actions

Cell permeable: yes
Primary Target
STAT3 pathway
Product does not compete with ATP.
Reversible: no
Target IC50: 5.6 and 3.7 µM in inhibiting malignant glioma growth in a viability assay using U87-MG and U373-MG, respectively

Disclaimer

Toxicity: Irritant (B)

General description

A cell-permeable AG 490 (Cat. No. 658401) tyrphostin analog that acts as an effective STAT3 pathway inhibitor and a much more potent antitumor agent than AG 490 in inhibiting malignant glioma growth both in cultures in vitro (IC50 = 5.6 and 3.7 µM in a viability assay using U87-MG and U373-MG, respectively; no inhibition against nontumor NHA at 10 µM) and in mice in vivo. Shown to cross blood-brain barrier in mice in vivo.
A cell-permeable AG 490 (Cat. No. 658401 ) tyrphostin analog that acts as an effective STAT3 pathway inhibitor and a much more potent antitumor agent than AG 490 in inhibiting malignant glioma growth both in cultures in vitro (IC50 = 5.6 and 3.7 µM in a viability assay using U87-MG and U373-MG, respectively; no inhibition against nontumor NHA at 10 µM) and in mice in vivo. Shown to cross blood-brain barrier in mice in vivo. Also available in InSolution format (Cat. No. 573129)

Other Notes

Iwamaru, A., et al. 2007. Oncogene,26, 2435.





Warning : This material may revert back to its native form.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Classe de stockage

11 - Combustible Solids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificats d'analyse (COA)

Recherchez un Certificats d'analyse (COA) en saisissant le numéro de lot du produit. Les numéros de lot figurent sur l'étiquette du produit après les mots "Lot" ou "Batch".

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Consulter la Bibliothèque de documents

Alicia Haydo et al.
EMBO reports, 24(12), e56964-e56964 (2023-11-08)
Glioblastoma is a very aggressive tumor and represents the most common primary brain malignancy. Key characteristics include its high resistance against conventional treatments, such as radio- and chemotherapy and its diffuse tissue infiltration, preventing complete surgical resection. The analysis of
In-Hye Ham et al.
International journal of oncology, 61(1) (2022-05-28)
The present study aimed to investigate whether the Janus‑activated kinase (JAK)/signal transducer and activator of transcription 3 (STAT3) signaling pathway is a critical mechanism underlying the cancer‑associated fibroblast (CAF)‑induced chemoresistance of gastric cancer (GC). In addition, the present study tried to
Eun-Ji Lim et al.
Cell death & disease, 13(4), 417-417 (2022-04-30)
Colorectal cancer (CRC) has a 5-year survival rate of <10%, as it can metastasize to the lungs and liver. Anticancer drugs and targeted therapies used to treat metastatic colorectal cancer have insufficient therapeutic efficacy and are associated with complications. Therefore
Meng Chi et al.
Annals of translational medicine, 8(8), 531-531 (2020-05-16)
Dexmedetomidine (DEX), a highly selective α2-adrenergic receptor agonist, has been reported to increase the malignancy of breast cancer cells in vitro and stimulate tumor growth in mice. Transmembrane protease serine 2 (TMPRSS2) demonstrates proteolytic activity, resulting in degradation of the
Ahmad Sharanek et al.
Cell reports, 36(9), 109647-109647 (2021-09-02)
Brain tumor stem cells (BTSCs) and intratumoral heterogeneity represent major challenges in glioblastoma therapy. Here, we report that the LGALS1 gene, encoding the carbohydrate binding protein, galectin1, is a key regulator of BTSCs and glioblastoma resistance to therapy. Genetic deletion
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Contenu apparenté

An Introduction to Inhibitors and Their Biological Applications - 1st Edition

An Introduction to Inhibitors and Their Biological Applications

JAK/STAT Signaling Research Focus

The Janus kinase (JAK)/signal transducers and activators of transcription (STAT) signaling pathway plays an important role in cell proliferation, cell differentiation, cell migration, and cell death. It is the principal signaling mechanism for a variety of cytokines and growth factors. Constitutive activation or dysregulation of JAK/STAT signaling can result in inflammatory disease, erythrocytosis, gigantism, and leukemia.

Pathways and Biomarkers of JAK/STAT Signaling

Pathways and Biomarkers of JAK/STAT Signaling

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