15 products were found matching "SYN-1023-M100"!

Soluble in DMSO or ethanol. Slightly soluble (<1mg/ml) in water.TAK-632 is a potent pan-RAF inhibitor with favorable in vitro activity (BRAF(V600E) IC(50) of 2.4nM. Target: Raf , Kinase Group: TKL , Substrate: Serine-Threonine

Solid. Soluble in DMSO or DMF. Selective PI3Kalpha inhibitor with IC50 of 5nM. Has minimal effect on other PI3K isoforms. Exhibits favorable pharmacokinetics and excellent oral bioavailability in animal models. In xenografts using nude mice, it showed dose-dependent effects of tumour inhibition. In a phase Ib study,...

Soluble in DMSO or ethanol. BX912 is a PDK1 (3-Phosphoinositide-dependent Kinase-1) inhibitor, with an IC(50) of 26nM. Target: PDK1 , Kinase Group: AGC , Substrate: Serine-Threonine

Soluble in DMSO or ethanol. The kinases called p38 MAP kinases (MAPKs) are intracellular, soluble serine-threonine kinases which belong to a large family of proteins that include the extracellular regulated kinases (ERKs) and c-Jun N-terminal kinases (JNKs). So far four p38 isoforms have been identified, namely...

Soluble in DMSO. Kinases, such as LIM kinase 1 (LIMK1) and LIM kinase 2 (LIMK2), have been identified as participating in signal pathways affecting actin dynamics by deactivating cofilin. Over expression of LMK1 has been found in invasive breast and prostate cancer cell lines and suppression of LIMK 2 expression has...

Soluble in DMSO. CC-401 is a competitive inhibitor of the ATP binding site in the active, phosphorylated, form of JNK. This prevents JNK from phosphorylating its various target molecules, including the amino terminus of c-Jun. It is a potent inhibitor of all three forms of JNK (Ki of 25-50 nM), and has at least...

Soluble in DMSO. Slightly soluble (<1mg/ml) in ethanol. Quizartinib (AC220) is a second-generation FLT3 inhibitor that has shown promising activity in AML in Phase II clinical trials. It inhibits mutant and wild-type FLT3 in vivo at 0.1 and 0.5µM, respectively, and has shown favorable activity and tolerability in...

Soluble in DMSO. Slightly soluble (<1mg/ml) in ethanol. Tivozanib is a potent inhibitor of VEGFR-1, 2 & 3 (IC(50) 0.21, 0.16 and 0.24nM respectively). Target: VEGFR , Kinase Group: RTK , Substrate: Tyrosine

Soluble in DMSO or ethanol. CP-724714 is an oral, selective and potent ErbB-2 (HER2) kinase inhibitor with an IC(50) of 10 nM. It has >640-fold selectivity for ErbB-2 (HER2) over EGFR, InsR, IRG-1R, PDGFR, VEGFR2, Abl, Src, c-Met. Target: HER2 , Kinase Group: RTK , Substrate: Tyrosine

Soluble in DMSO. SR-3677 had an IC(50) of approximately 3nM in enzyme and cell based assays and had an off-target hit rate of 1.4% against 353 kinases, and inhibited only 3 out of 70 non-kinase enzymes and receptors. Pharmacology studies showed that 5 was efficacious in both, increasing ex vivo aqueous humor outflow...

Soluble in DMSO. Slightly soluble (<1mg/ml) in ethanol. BI-D1870 is a small molecule, specific inhibitor of p90 RSK (ribosomal S6 kinase) isoforms RSK1, RSK2, RSK3 and RSK4, both in vitro and in vivo, with IC(50)s are 31nM, 24nM, 18nM, 15nM, respectively. It shows a 10- to 100-fold selectivity for RSK over MST2,...

Soluble in DMSO or ethanol. BX795 was initially developed as a PDK1 inhibitor (direct competitive inhibitor IC(50) 11nM for PDK1) and has been shown to be a potent and relatively specific inhibitor of TBK1 and IKK-epsilon. It blocks the phosphorylation, nuclear translocation, and transcriptional activity of...