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ARQ-197 has been shown to prevent HGF/c-met induced cellular responses in vitro. ARQ-197 possesses antitumor activity; inhibiting proliferation of A549, DBTRG and NCI-H441 cells with IC50 of 0.38, 0.45, 0.29 ¦ÌM. Treatment with ARQ-197 results in a decrease in phosphorylation of the MAPK signaling cascade and prevention of invasion and migration. In addition, ectopic expression of c-Met in NCI-H661, a cell line having no endogenous expression of c-Met, causes it to acquire an invasive phenotype that is also suppressed by ARQ-197. Although the addition of increasing concentrations of ARQ-197 does not significantly affect the Km of ATP, exposure of c-Met to 0.5 ¦ÌM ARQ-197 decreased the Vmax of c-Met by approximately 3-fold. The ability of ARQ-197 to decrease the Vmax without affecting the Km of ATP confirmed that ARQ-197 inhibits c-Met through a non¨CATP-competitive mechanism and may therefore account for its high degree of kinase selectivity. ARQ-197 prevents human recombinant c-Met with a calculated inhibitory constant Ki of approximately 355 nM. Although the highest concentration of ATP used is 200 ¦ÌM, the potency of ARQ-197 against c-Met is not reduced by using concentrations of ATP up to 1 mM. ARQ-197 blocks c-Met phosphorylation and downstream c-Met signaling pathways. ARQ-197 suppresses constitutive and ligand-mediated c-Met autophosphorylation and, by extension, c-Met activity, in turn leading to the inhibition of downstream c-Met effectors. ARQ-197 induction of caspase-dependent apoptosis is increased in c-Met¨Cexpressing human cancer cells including HT29, MKN-45, and MDA-MB-231 cells

June 21, 2017

prudect name : ARQ-197 has been shown to prevent HGF/c-met induced cellular responses in vitro. ARQ-197 possesses antitumor activity; inhibiting proliferation of A549, DBTRG and NCI-H441 cells with IC50 of…

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PD0332991£¨Palbociclib) Intermediates

prudect name : PD0332991£¨Palbociclib) Intermediatestert-Butyl 4-(6-aminopyridin-3-yl)piperazine-1-carboxylate Synonyms: CAS NO: 571188-59-5Molecular Formula: C14H22N4O2Molecular Weight: 278.35Purity: 98% minSolubility: in DMSOStorage: -20oC web site: www.medchemexpress.com

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TCS JNK 5a(JNK Inhibitor IX) is a selective inhibitor of JNK2 and JNK3 (pIC50 values are 6.7, 6.5, <5.0 and <4.8 for JNK3, JNK2, JNK1 and p38¦Á respectively); displays no significant activity at a range of other protein kinases including EGFR, ErbB2, cdk2,

prudect name : TCS JNK 5a(JNK Inhibitor IX) is a selective inhibitor of JNK2 and JNK3 (pIC50 values are 6.7, 6.5,

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TAK-632 is a selective pan-RAF kinase inhibitor with IC50 values of 2.4/1.4 nM for BRAF V600E/c-RAF; > 60 fold selectivity over VEGFR.

prudect name : TAK-632 is a selective pan-RAF kinase inhibitor with IC50 values of 2.4/1.4 nM for BRAF V600E/c-RAF; > 60 fold selectivity over VEGFR.TAK 632;TAK-632;TAK632 Synonyms: CAS NO: 1228591-30-7Molecular…

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Triciribine is a synthetic tricyclic nucleoside which acts as a specific inhibitor of the Akt signaling pathway. It selectively inhibits the phosphorylation and activation of Akt1, -2 and -3 but does not inhibit Akt kinase activity nor known upstream Akt activators such as PI 3-Kinase and PDK1. It inhibits cell growth and induces apoptosis preferentially in cells that express aberrant Akt. This agent is shown≥ 80% inhibition in tumor growth in mice at 1 mg/kg/day, i.p.

prudect name : Triciribine is a synthetic tricyclic nucleoside which acts as a specific inhibitor of the Akt signaling pathway. It selectively inhibits the phosphorylation and activation of Akt1, -2…

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prudect name : TOK-001Synonyms: VN124-1CAS NO: 851983-85-2Molecular Formula: C26H32N2OMolecular Weight: 388.55Purity: 98% minSolubility: In DMSOStorage:

prudect name : TOK-001 Synonyms: VN124-1CAS NO: 851983-85-2Molecular Formula: C26H32N2OMolecular Weight: 388.55Purity: 98% minSolubility: In DMSOStorage: -20°C web site: www.medchemexpress.com

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N-[(4-aminophenyl)carbamothioyl]-4-tert-butylbenzamide

prudect name : N-[(4-aminophenyl)carbamothioyl]-4-tert-butylbenzamideTenovin-3 Synonyms: CAS NO: 1011301-27-1Molecular Formula: C18H21N3OSMolecular Weight: 327.444Purity: 98% minSolubility: in DMSOStorage: -20oC web site: www.medchemexpress.com

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TG100-115 is applied to anti-inflammatory therapy for respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD). TG100-115 could reduce inflammation and mucin accumulation.

prudect name : TG100-115 is applied to anti-inflammatory therapy for respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD). TG100-115 could reduce inflammation and mucin accumulation.TG100-115 Synonyms: CAS…

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Tenovin-6 is the water soluble analog of Tenovin-1 (HY-13423) and acts as a potent SIRT1 (IC50=21 uM) and SIRT2 (IC50= 10 uM) inhibitor as well as p53 activator.

prudect name : Tenovin-6 is the water soluble analog of Tenovin-1 (HY-13423) and acts as a potent SIRT1 (IC50=21 uM) and SIRT2 (IC50= 10 uM) inhibitor as well as p53…

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prudect name : Torin 2Synonyms: CAS NO: 1223001-51-1Molecular Formula: C24H15F3N4OMolecular Weight: 432.40Purity: 98%Solubility: In DMSOStorage:

prudect name : Torin 2 Synonyms: CAS NO: 1223001-51-1Molecular Formula: C24H15F3N4OMolecular Weight: 432.40Purity: 98%Solubility: In DMSOStorage: -20°C web site: www.medchemexpress.com

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