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AZD8330 potently and strongly inhibits MEK 1/2. AZD8330 has no inhibitory activity against over 200 other kinases including at concentrations up to 10 ¦ÌM. AZD8330 demonstrates sub-nanomolar potency in mechanistic (pERK) and low to sub-nanomolar potency in functional (proliferation) assays in MEK 1/2 inhibitor sensitive cell lines.

June 21, 2017

prudect name : AZD8330 potently and strongly inhibits MEK 1/2. AZD8330 has no inhibitory activity against over 200 other kinases including at concentrations up to 10 ¦ÌM. AZD8330 demonstrates sub-nanomolar…

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Acalabrutinib is a potent and selective BTK (Bruton¡¯s tyrosine kinase) inhibitor. BTK is a cytoplasmic, non-receptor tyrosine kinase that transmits signals from a variety of cell-surface molecules, including the B-cell receptor (BCR) and tissue homing receptors. Genetic BTK deletion causes B-cell immunodeficiency in humans and mice, making this kinase an attractive therapeutic target for B-cell disorders. BTK inhibitors targeting B cell receptor signaling and other survival mechanism showed great promise for the treatment of chronic lymphocytic leukemia (CLL)s holds great promise.

prudect name : Acalabrutinib is a potent and selective BTK (Bruton¡¯s tyrosine kinase) inhibitor. BTK is a cytoplasmic, non-receptor tyrosine kinase that transmits signals from a variety of cell-surface molecules,…

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Apixaban is a highly selective, reversible inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively.

prudect name : Apixaban is a highly selective, reversible inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively.Apixaban Synonyms: CAS NO: 503612-47-3Molecular…

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AP26113 is a potent ALK inhibitor with IC50 of 0.62 nM in a cell-free assay, demonstrated ability overcome Crizotinib resistance mediated by a L1196M mutation. Phase 2.

prudect name : AP26113 is a potent ALK inhibitor with IC50 of 0.62 nM in a cell-free assay, demonstrated ability overcome Crizotinib resistance mediated by a L1196M mutation. Phase 2.AP26113…

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A 83-01 is a selective inhibitor of TGF-_beta_ type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7 (IC50 values are 12, 45 and 7.5 nM respectively).

prudect name : A 83-01 is a selective inhibitor of TGF-_beta_ type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7 (IC50 values are…

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AT-406 is a Smac mimetic and appears to mimic closely the AVPI peptide in both hydrogen bonding and hydrophobic interactions with XIAP, with additional hydrophobic contacts with W323 of XIAP. AT-406 is more sensitive to these IAPs than Smac AVPI peptide with 50-100 fold binding affinities. AT-406 (at 1 ¦ÌM) completely restores the activity of caspase-9, which is suppressed by 500 nM XIAP BIR3 in a cell-free system. In MDA-MB-231 cell, AT-406 induces rapid cellular cIAP1 degradation and also pulls down the cellular XIAP protein. AT-406 effectively inhibits lots of human cancer cell lines and shows IC50 of 144 and 142 nM in MDA-MB-231 cell and SK-OV-3 ovarian cell, with low toxicity against normal-like human breast epithelial MCF-12F cells and primary human normal prostate epithelial cells. AT-406 induces apoptosis in MDA-MB-231 cell by inducing activation of caspase-3 and cleavage of PARP.

prudect name : AT-406 is a Smac mimetic and appears to mimic closely the AVPI peptide in both hydrogen bonding and hydrophobic interactions with XIAP, with additional hydrophobic contacts with…

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AZD5363 is an orally active, selective protein kinase B (PKB, also known as Akt) inhibitor derived from a collaborative drug discovery program between AstraZeneca, Astex Pharmaceuticals™, The Institute of Cancer Research (ICR) and Cancer Research Technology Limited (CRT). The program began in 2003 through Astex Pharmaceuticals¡¯ collaboration with ICR and CRT, and AstraZeneca¡¯s collaboration with Astex Pharmaceuticals on a drug discovery program targeting PKB/Akt began in 2005. Inhibition of the PKB/Akt pathway has potential in the treatment of a broad range of tumor types. In April 2011 AstraZeneca announced that it had commenced a phase 1 study of AZD5363 in patients with advanced solid tumors.

prudect name : AZD5363 is an orally active, selective protein kinase B (PKB, also known as Akt) inhibitor derived from a collaborative drug discovery program between AstraZeneca, Astex Pharmaceuticals™, The…

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prudect name : AG1024Synonyms: CAS NO: 65678-07-1Molecular Formula: C14H13BrN2OMolecular Weight: 305.174Purity: 98% minSolubility: In DMSOStorage:

prudect name : AG1024 Synonyms: CAS NO: 65678-07-1Molecular Formula: C14H13BrN2OMolecular Weight: 305.174Purity: 98% minSolubility: In DMSOStorage: −20°C 187164-19-8 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18500921

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AMG 925 is a potent and selective dual inhibtor of CDK4/FLT3 with IC50s of 1.5 nM and 2.4 nM for CDK4 and FLT3, respectively; with IC50 of 19 nM in MOLM-13 cell. IC50 value: 1.5/2.4 nM (CDK4/FLT3)

prudect name : AMG 925 is a potent and selective dual inhibtor of CDK4/FLT3 with IC50s of 1.5 nM and 2.4 nM for CDK4 and FLT3, respectively; with IC50 of…

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AMG 319 is an investigational, highly selective, small molecule inhibitor of PI3K¦Ä that blocks B cell proliferation following BCR stimulation both in vitro and in vivo, inhibits basal AKT phosphorylation, and inhibits proliferation in lymphoid tumor cells.

prudect name : AMG 319 is an investigational, highly selective, small molecule inhibitor of PI3K¦Ä that blocks B cell proliferation following BCR stimulation both in vitro and in vivo, inhibits…

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