573097
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.
Synonym(s):
STAT3 Inhibitor III, WP1066
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About This Item
Empirical Formula (Hill Notation):
C17H14BrN3O
CAS Number:
Molecular Weight:
356.22
UNSPSC Code:
12352200
NACRES:
NA.77
Quality Level
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
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
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. Also available in InSolution format (Cat. No. 573129.
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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
STAT3 pathway
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
Packaging
Packaged under inert gas
Warning
Toxicity: Irritant (B)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Iwamaru, A., et al. 2007. Oncogene,26, 2435.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
WGK
WGK 2
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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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
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
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
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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