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509105 STAT3/STAT5 Dual Inhibitor, SH-4-54 - CAS 1456632-40-8 - Calbiochem

509105
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Aperçu

Replacement Information

Tableau de caractéristiques principal

CAS #Empirical Formula
1456632-40-8C₂₉H₂₇F₅N₂O₅S

Products

RéférenceConditionnement Qté
5091050001 Flacon en verre 10 mg
Description
OverviewA cell-permeable BP-1-102 (Cat. no. 573132) analog that targets STAT3 and STAT5 with comparable affinity and is 4-fold more potent in competing against phosphopeptide for binding SH2 domain of STAT3 over STAT1, exhibiting little potency against upstream kinases or the activation of 21 GPCRs, and displaying much reduced or no affinity toward other kinases in a 101-panel screen. Selectively inhibits cellular STAT3 Y705, but not S727, phosphorylation (0.5 to 5 µM) and is a more potent anticancer agent than BP-1-102 against gliobalstoma (GMB) patients-derived brain tumor stem cell (BTSC) in cultures (IC50 from 42 to 530 nM). Reported to penetrate blood-brain-barrier in mice and effectively inhibit BT73 glioma proliferation in xenografted murine brain (10 mg/kg/d via i.p.; 4 d on/ 3 d off) in vivo.
Catalogue Number509105
Brand Family Calbiochem®
SynonymsSTAT3 Inhibitor XIX, STAT5 Inhibitor IV, 4-(N-(4-Cyclohexylbenzyl)-2-(2,3,4,5,6-pentafluoro-N-methylphenylsulfonamido)acetamido)benzoic acid, SH-04-54, SH0454, SH454
References
ReferencesHaftchenary, S., et al. 2013. ACS Med. Chem. Lett. 4, In press.
Product Information
CAS number1456632-40-8
FormWhite powder
Hill FormulaC₂₉H₂₇F₅N₂O₅S
Chemical formulaC₂₉H₂₇F₅N₂O₅S
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetSTAT3
Secondary targetSTAT5
Purity≥94% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Référence GTIN
5091050001 04055977261486

Documentation

STAT3/STAT5 Dual Inhibitor, SH-4-54 - CAS 1456632-40-8 - Calbiochem FDS

Titre

Fiche de données de sécurité des matériaux (FDS) 

STAT3/STAT5 Dual Inhibitor, SH-4-54 - CAS 1456632-40-8 - Calbiochem Certificats d'analyse

TitreNuméro de lot
509105

Références bibliographiques

Aperçu de la référence bibliographique
Haftchenary, S., et al. 2013. ACS Med. Chem. Lett. 4, In press.

Informations techniques

Titre
JAK/STAT Signaling Research Focus
Fiche technique

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision21-February-2014 JSW
SynonymsSTAT3 Inhibitor XIX, STAT5 Inhibitor IV, 4-(N-(4-Cyclohexylbenzyl)-2-(2,3,4,5,6-pentafluoro-N-methylphenylsulfonamido)acetamido)benzoic acid, SH-04-54, SH0454, SH454
DescriptionA cell-permeable, salicyclic-to-benzoic acid-substituted BP-1-102 (Cat. no. 573132) analog that targets STAT3 and STAT5 with comparable affinity (koff/kon = KD = 300 and 464 nM, respectively) and is 4-fold more potent in competing against phosphopeptide for binding to SH2 domain of STAT3 over STAT1 (Ki = 23.5 and 92.3 µM, respectively; [phosphopeptide] = 10 nM), exhibiting little potency against the kinase activity of upstream kinases (Akt1, Erk1, JAK1/2, c-Src) or the activation of 21 GPCRs, and displaying much reduced or no affinity toward other kinases in a 101-panel screen. Selectively inhibits cellular STAT3 Y705, but not S727, phosphorylation (0.5 to 5 µM) and is a more potent anticancer agent than BP-1-102 against gliobalstoma (GMB) patients-derived brain tumor stem cell (BTSC) cultures (IC50 from 42 to 530 nM). Reported to penetrate blood-brain-barrier in mice (Conc in brain = 313 nM 30 min post 10 mg/kg i.p. dosing) and effectively inhibit BT73 glioma proliferation in xenografted murine brain via apoptosis induction (10 doses: 10 mg/kg i.p., 4 d on/ 3 d off) in vivo.
FormWhite powder
Intert gas (Yes/No) Packaged under inert gas
CAS number1456632-40-8
Chemical formulaC₂₉H₂₇F₅N₂O₅S
Structure formulaStructure formula
Purity≥94% by HPLC
SolubilityDMSO (100 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesHaftchenary, S., et al. 2013. ACS Med. Chem. Lett. 4, In press.