A multi-kinase inhibitor; inhibits TrkA

TPX-0005 – 5 mg

Brand:
Cayman
CAS:
1802220-02-5
Storage:
-20
UN-No:
De Minimis - 3077 / 9

TPX-0005 is a multi-kinase inhibitor that inhibits TrkA, TrkB, and TrkC (IC50s = 0.83, 0.05, and 0.1 nM, respectively) as well as C-ros oncogene 1 (ROS1; IC50 = 0.07 nM).{36850} It inhibits a variety of other kinases, including ALK, JAK2, LYN, Src, and FAK (IC50s = 1.04, 1.04, 1.66, 5.3, and 6.96 nM, respectively). It inhibits proliferation of PC-9, H1975, 11-18, HCC4006, and HCC827 lung cancer cells (IC50s = 100, 100, 150, 148, and 430 nM, respectively) with additive or synergistic effects when used in combination with gefitinib (Item No. 13166), afatinib (Item No. 11492), PF-299804 (dacomitinib; Item No. 9001879), or osimertinib. TPX-0005 (30 mg/kg) reduces tumor growth in PC-9 and H1975 mouse xenograft models and potentiates the effect of osimertinib in these models.  

 

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SKU: 23397 - 5 mg Category:

Description

A multi-kinase inhibitor; inhibits TrkA, TrkB, and TrkC (IC50s = 0.83, 0.05, and 0.1 nM, respectively) as well as ROS1 (IC50 = 0.07 nM); inhibits a variety of other kinases, including ALK, JAK2, LYN, Src, and FAK (IC50s = 1.04, 1.04, 1.66, 5.3, and 6.96 nM, respectively); inhibits proliferation of PC-9, H1975, 11-18, HCC4006, and HCC827 cells (IC50s = 100, 100, 150, 148, and 430 nM, respectively) with additive or synergistic effects when used in combination with certain compounds, including osimertinib; reduces tumor growth in PC-9 and H1975 mouse xenograft models; potentiates the effect of osimertinib on tumor growth in vivo

Formal name: (7S,13R)-11-fluoro-6,7,13,14-tetrahydro-7,13-dimethyl-1,15-etheno-1H-pyrazolo[4,3-f][1,4,8,10]benzoxatriazacyclotridecin-4(5H)-one

Synonyms: 

Molecular weight: 355.4

CAS: 1802220-02-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Receptor Tyrosine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|ALK (Activin-like Kinase) Signaling||Research Area|Cancer|Cell Signaling|JAK/STAT Signaling||Research Area|Cancer|Cell Signaling|SRC Family Signaling

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