KX2-391 (Tirbanibulin) - Moligand™, 10mM in DMSO , Tyrosine-protein kinase SRC inhibitor, CAS No.897016-82-9, Tyrosine-protein kinase SRC inhibitor

CAS: 897016-82-9 Cat. No.: K408930 Summenformel: C₂₆H₂₉N₃O₃ Molekulargewicht: 431.53 EG-Nummer: 854-810-1

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

KX 01 | N-benzyl-2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)acetamide

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Übersicht

Information

KX2-391 (Tirbanibulin) KX2-391, the first clinical Src inhibitor (peptidomimetic class) that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines. Phase 2.
In vitro

KX2-391 is a Src inhibitor that is directed to the Src substrate pocket. KX2-391 shows steep dose-response curves against Huh7 (GI 50 = 9 nM), PLC/PRF/5 (GI 50 = 13 nM), Hep3B (GI 50 = 26 nM), and HepG2 (GI 50 = 60 nM), four hepatic cell cancer (HCC) cell lines. KX2-391 is found to inhibit certain leukemia cells that are resistant to current commercially available drugs, such as those derived from chronic leukemia cells with the T3151 mutation. KX2-391 is evaluated in engineered Src driven cell growth assays inNIH3T3/c-Src527F and SYF/c-Src527F cells and exhibits GI50 with 23 nM and 39 nM, respectively.

In vivo

In pre-clinical animal models of cancer, orally administered KX2-391 is shown to inhibit primary tumor growth and to suppress metastasis.
Cell Data

cell lines：

Concentrations：6,564 to 0.012 nM

Incubation Time：3 days

Powder Purity:≥99%

Specifications

Synonyme

KX 01 | N-benzyl-2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)acetamide

Spezifikationen & Reinheit

Moligand™, 10mM in DMSO

Biochemische und physiologische Mechanismen

KX2-391, the first clinical Src inhibitor (peptidomimetic class) that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines. Phase 2.

Storage

Store at -80°C

Verschickt in

Dry ice packs + Cold packs

Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.

Note

Moligand™

Aktionsart

INHIBITOR

Mechanismus der Wirkung

Tyrosine-protein kinase SRC inhibitor

Produkteigenschaften

• ALogP: 2.9

Namen und Kennungen

• Isomere SMILES: C1COCCN1CCOC2=CC=C(C=C2)C3=CN=C(C=C3)CC(=O)NCC4=CC=CC=C4
• Molekulargewicht: 431.53
• Reaxy-Rn: 12650942
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=12650942&ln=

Zugehörige Ziele (menschlich)

SRC Tclin Proto-oncogene tyrosine-protein kinase Src (4 Activities)

Discover Target: SRC

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)