XL388 is a Novel Class of Highly Potent, Selective, ATP-Competitive, and Orally Bioavailable Inhibitors of the Mammalian Target of Rapamycin (mTOR). XL388 inhibited cellular phosphorylation of mTOR complex 1 (p-p70S6K, pS6, and p-4E-BP1) and mTOR complex 2 (pAKT (S473)) substrates. XL388 displayed good pharmacokinetics and oral exposure in multiple species with moderate bioavailability. Oral administration of XL388 to athymic nude mice implanted with human tumor xenografts afforded significant and dose-dependent antitumor activity.

 June 21, 2017

prudect name : XL388 is a Novel Class of Highly Potent, Selective, ATP-Competitive, and Orally Bioavailable Inhibitors of the Mammalian Target of Rapamycin (mTOR). XL388 inhibited cellular phosphorylation of mTOR…

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XL647 is an orally bioavailable small-molecule receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity. XL647 binds to and inhibits several tyrosine receptor kinases that play major roles in tumor cell proliferation and tumor vascularization, including epidermal growth factor receptor (EGFR; ERBB1), epidermal growth factor receptor 2 (HER2; ERBB2), vascular endothelial growth factor receptor (VEGFR), and ephrin B4 (EphB4). This may result in the inhibition of tumor growth and angiogenesis, and tumor regression.

prudect name : XL647 is an orally bioavailable small-molecule receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity. XL647 binds to and inhibits several tyrosine receptor kinases that play major…

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XMD8-92 is highly selective ERK5/BMK1 inhibitor (KD values are 80, 190, 600 and 890 nM for BMK1, DCAMKL2, PLK4 and TNK1 respectively). XMD8-92 displays selectivity over 402 diverse kinases. XMD8-92 blocks growth factor-induced activation of cellular BMK1 and reduces BMK1 activity in in vitro kinase assays. XMD8-92 also reduces BMK1-dependent transactivating activity of MEF2C. XMD8-92 inhibits proliferation in a variety of cancer cell lines; blocks tumor cell proliferation and tumor-associated angiogenesis.

prudect name : XMD8-92 is highly selective ERK5/BMK1 inhibitor (KD values are 80, 190, 600 and 890 nM for BMK1, DCAMKL2, PLK4 and TNK1 respectively). XMD8-92 displays selectivity over 402…

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Chemical Name: N1,N4-Di-2-pyridinyl-1,4-benzenedimethanamine

prudect name : Chemical Name: N1,N4-Di-2-pyridinyl-1,4-benzenedimethanamineWZ 811 Synonyms: CAS NO: 55778-02-4Molecular Formula: C18H18N4Molecular Weight: 290.36Purity: 98% minSolubility: In DMSOStorage: −20°C web site: www.medchemexpress.com

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WS6 is a novel small molecule that promotes ¦Â cell proliferation in rodent and human primary islets with EC50 of 0.28 uM(R7T1 cell viability).

prudect name : WS6 is a novel small molecule that promotes ¦Â cell proliferation in rodent and human primary islets with EC50 of 0.28 uM(R7T1 cell viability).WS6;WS-6;WS-6 Synonyms: CAS NO:…

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WH-4-023 is a potent and selective dual Lck/Src inhibitor with IC50 of 2 nM/6 nM for Lck and Src kinase respectively; little inhibition on p38¦Á and KDR.

prudect name : WH-4-023 is a potent and selective dual Lck/Src inhibitor with IC50 of 2 nM/6 nM for Lck and Src kinase respectively; little inhibition on p38¦Á and KDR.WH-4-023…

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WAY-100635 is a potent and selective 5-hydroxytryptamine1A antagonist with an IC50 of 0.95 ¡À 0.12 nM for 5-HT. Intravenous administration of WAY-100635 (0.025-0.5 mg/kg) markedly improved neuronal activity. The stimulatory action of WAY-100635 was evident during wakefulness (when serotonergic neurons typically display a relatively high level of activity) but not during sleep (when serotonergic neurons display little or no spontaneous activity). WAY-100635 at doses as low as 0.1 mg/kg i.v. completely blocked the action of 8-hydroxy-2-(di-n-propylamino)tetralin. The antagonist action of WAY-100635 at 5-HT1A autoreceptors closely paralleled its ability to increase neuronal activity.

prudect name : WAY-100635 is a potent and selective 5-hydroxytryptamine1A antagonist with an IC50 of 0.95 ¡À 0.12 nM for 5-HT. Intravenous administration of WAY-100635 (0.025-0.5 mg/kg) markedly improved neuronal…

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WYE-125132 is a highly potent, ATP-competitive and specific mTOR kinase inhibitor with an IC50 of 0.19 nM. WYE-125132 blocked the activity of the both of mTORC1 and mTORC2 in various models of cancer in vitro and in vivo. WYE-125132 is 5,000-fold more selective than PI3Ks. Moreover, WYE-125132 completely blocked amino acid-induced phosphorylation of Maf1, just as S6K1, and 4E-BP1 via the inhibition of mTOR. WYE-132-treated MG63 markedly upregulated the Maf1 amouts in the nucleus. WYE-125132 showed a substantially more effective inhibition in many respects, including cancer cell growth and survival, protein synthesis bioenergetic metabolism, and adaptation to hypoxia by contrast with the rapalog temsirolimus/CCI-779.

prudect name : WYE-125132 is a highly potent, ATP-competitive and specific mTOR kinase inhibitor with an IC50 of 0.19 nM. WYE-125132 blocked the activity of the both of mTORC1 and…

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WZ4002 inhibits other EGFR genotypes E746_A750 and E746_A750/T790M with IC50 of 2 and 6 nM. Besides, WZ4002 suppresses widetype ERBB2 with an IC50 of 32 nM. WZ4002 inhibits EGFR, AKT and ERK1/2 phosphorylation in NSCLC cell lines and WZ4002 prevents of EGFR phosphorylation in NIH-3T3 cells expressing different EGFR T790M mutant alleles. For WZ4002, kinases that exhibited greater than 95% inhibition relative to the DMSO control at 10 ¦ÌM are selected for measurement of their dissociation constants. WZ4002, which possesses an ortho-methoxy group at the C2-aniline substituent, is more selective for EGFR compared to WZ3146. WZ4002 is 100-fold less effective at inhibiting phosphorylation of WT EGFR compared to the quinazoline inhibitors. Similarly, WZ4002 prevents EGFR kinase activity of recombinant L858R/T790M protein more potently than of WT EGFR, while the opposite is observed with HKI-272 and gefitinib.

prudect name : WZ4002 inhibits other EGFR genotypes E746_A750 and E746_A750/T790M with IC50 of 2 and 6 nM. Besides, WZ4002 suppresses widetype ERBB2 with an IC50 of 32 nM. WZ4002…

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WS3 is a novel small molecule that promotes ¦Â cell proliferation with EC50 of 28 nM(induced R7T1 proliferation).

prudect name : WS3 is a novel small molecule that promotes ¦Â cell proliferation with EC50 of 28 nM(induced R7T1 proliferation).WS3;WS-3;WS 3 Synonyms: CAS NO: 1421227-52-2Molecular Formula: C28H30F3N7O3Molecular Weight: 569.58Purity:…

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