prudect name : Glycine isopropyl ester hydrochlorideSynonyms: CAS NO: 14019-62-6Molecular Formula: C5H12ClNO2Molecular Weight: 153.61Purity: 98%

 June 21, 2017

prudect name : Glycine isopropyl ester hydrochloride Synonyms: CAS NO: 14019-62-6Molecular Formula: C5H12ClNO2Molecular Weight: 153.61Purity: 98% minSolubility: Storage: −20°C LEE 011 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18516045

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I-BET151(GSK1210151A) is identified and optimized to retain excellent BET target potency and selectivity while enhancing the in vivo pharmacokinetics and terminal half-life to enable prolonged in vivo studies.

prudect name : I-BET151(GSK1210151A) is identified and optimized to retain excellent BET target potency and selectivity while enhancing the in vivo pharmacokinetics and terminal half-life to enable prolonged in vivo…

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prudect name : GW 501516Synonyms: CAS NO: 317318-70-0Molecular Formula: C21H18F3NO3S2Molecular Weight: 453.50Purity: 98% minSolubility: In

prudect name : GW 501516 Synonyms: CAS NO: 317318-70-0Molecular Formula: C21H18F3NO3S2Molecular Weight: 453.50Purity: 98% minSolubility: In DMSOStorage: -20°C GSK-2334470 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/1851597

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GSK1120212 (JTP-74057) is a reversible, selective, allosteric MEK1/MEK2 kinase activity inhibitor with IC50 of 0.7 and 0.9 nM for MEK1 and MEK2.GSK1120212 (JTP-74057) strongly prevented the activities of MEK1 and MEK2 kinases rather than activities of other 98 kinases. After treatment of GSK1120212 (JTP-74057), it led to the growth inhibition and upregulate p15INK4b and/or p27KIP1 in most of the colorectal cancer cell lines tested. In nude animal mice studies, JTP-74057 inhibited tumor growth of HT-29 and COLO205 xenografts when GSK1120212 (JTP-74057) was daily oral administered for 14 days. GSK1120212 (JTP-74057) showed an additive or a synergistic action in combination with the standard-of-care agents, 5-fluorouracil, oxaliplatin or SN-38. Sensitivity to JTP-74057-induced apoptosis may be an important factor for the estimation of in vivo efficacy, and sensitivity was enhanced by an Akt inhibitor.GSK1120212 (JTP-74057) is originally developed by GlaxoSmithKline and is recruiting for phase I clinical trials for the treatment of solid tumors.

prudect name : GSK1120212 (JTP-74057) is a reversible, selective, allosteric MEK1/MEK2 kinase activity inhibitor with IC50 of 0.7 and 0.9 nM for MEK1 and MEK2.GSK1120212 (JTP-74057) strongly prevented the activities…

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Geldanamycin is a benzoquinone ansamycin antibiotic that binds to Hsp90 (Heat Shock Protein 90) and alters its function. Geldanamycin induces the degradation of proteins that are mutated in tumor cells such as v-Src, Bcr-Abl and p53 preferentially over their normal cellular counterparts. This effect is mediated via HSP90. Despite its potent antitumor potential, geldanamycin presents several major drawbacks as a drug candidate (namely, hepatotoxicity) that have led to the development of geldanamycin analogues, in particular analogues containing a derivatisation at the 17 position:17-AAG，17-DMAG.

prudect name : Geldanamycin is a benzoquinone ansamycin antibiotic that binds to Hsp90 (Heat Shock Protein 90) and alters its function. Geldanamycin induces the degradation of proteins that are mutated…

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prudect name : Gabapentin hydrochlorideSynonyms: CAS NO: 60142-96-3Molecular Formula: C9H17NO2.HCl;C9H18ClNO2Molecular Weight: 207.70Purity: ≥99%Solubility: Storage: −20°C

prudect name : Gabapentin hydrochloride Synonyms: CAS NO: 60142-96-3Molecular Formula: C9H17NO2.HCl;C9H18ClNO2Molecular Weight: 207.70Purity: ≥99%Solubility: Storage: −20°C 2 years ZM 241385 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18515863

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GW788388 shows anti-TGF-¦Â activity with IC50 of 93 nM in cellular assay.GW788388 shows some inhibitory to activin type II receptor (ActRII) but no inhibitory to bone morphogenic protein (BMP) type II receptor. GW788388 shows no toxicity in Namru murine mammary gland (NMuMG), MDA-MB-231, renal cell carcinoma (RCC)4, and U2OS cells at 4 nM to 15 ¦ÌM. GW788388 blocks TGF-¦Â-induced Smad activation and target gene expression, while decreasing epithelial¨Cmesenchymal transitions and fibrogenesis. GW788388 inhibits ALK5, ALK4, ALK7 and TGF-¦Â-mediated growth arrest.

prudect name : GW788388 shows anti-TGF-¦Â activity with IC50 of 93 nM in cellular assay.GW788388 shows some inhibitory to activin type II receptor (ActRII) but no inhibitory to bone morphogenic…

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GDC-0973(XL-518; GDC 0973) is a selective inhibitor of MEK. GDC-0973 is also known as mitogen activated protein kinase kinase (MAPKK), is a key component of the RAS/RAF/MEK/ERK pathway, which is frequently activated in human tumors. Inappropriate activation of the MEK/ERK pathway promotes cell growth in the absence of exogenous growth factors.

prudect name : GDC-0973(XL-518; GDC 0973) is a selective inhibitor of MEK. GDC-0973 is also known as mitogen activated protein kinase kinase (MAPKK), is a key component of the RAS/RAF/MEK/ERK…

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GDC-0980 (RG7422) is a selective, dual PI3 Kinase and mTOR Kinase inhibitor with IC50 of 5, 27, 7, and 14 nM for PI3K¦Á, ¦Â, ¦Ä, and ¦Ã, respectively. PI3 Kinase is an oncogene which is commonly mutated in cancer. The PI3K/Akt/mTOR signaling pathway modulates cell growth and survival and play a crucial role downsream of KIT signaling. GDC-0980 (RG7422) prevents mTOR with a Ki of 17 nM. GDC-0980 (RG7422) is highly selective versus a large panel of kinases including others in the PIKK family. GDC-0980 (RG7422) possesses robust activity and excellent pharmacokinetic and pharmaceutical properties in cancer models driven by the PI3K pathway. GDC-0980 potently prevents signal transduction downstream of both PI3K and mTOR, as measured by pharmacodynamic (PD) biomarkers, thereby acting upon two key pathway nodes to produce the strongest attainable inhibition of signaling in the pathway. Correspondingly, GDC-0980 (RG7422) was potent across a broad panel of cancer cell lines, with the greatest potency in breast, prostate, and lung cancers and less activity in melanoma and pancreatic cancers, consistent with KRAS and BRAF acting as resistance markers. Treatment of cancer cell lines with GDC-0980 resulted in G1 cell cycle arrest, and in contrast to mTOR inhibitors, Correspondingly triggered apoptosis in certain cancer cell lines, including those with direct pathway activation via PI3K and PTEN. Low doses of Correspondingly potently suppressed tumor growth in xenograft models including those with activated PI3K, loss of LKB1 or PTEN, and elicited an exposure-related decrease in PD biomarkers. On the basis of the cell potency, low clearance in mouse, and high free fraction, 2 demonstrated significant efficacy in mouse xenografts when dosed as low as 1 mg/kg orally and is currently in phase I clinical trials for cancer.GDC-0980 (RG7422) is originally developed by Genentech. The phase I clinical trials for GDC0980 is currently recruiting participants.

prudect name : GDC-0980 (RG7422) is a selective, dual PI3 Kinase and mTOR Kinase inhibitor with IC50 of 5, 27, 7, and 14 nM for PI3K¦Á, ¦Â, ¦Ä, and ¦Ã,…

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GDC-0449 (Vismodegib) is a more potent novel and specific synthetic oral hedgehog pathway inhibitor with an IC50 of 3 nM. It targets the Hedgehog signaling pathway, blocking the activities of the Hedgehog-ligand cell surface receptors PTCH and/or SMO and suppressing Hedgehog signaling. The Hedgehog signaling pathway plays an important role in tissue growth and repair; aberrant constitutive activation of Hedgehog pathway signaling and uncontrolled cellular proliferation may be associated with mutations in the Hedgehog-ligand cell surface receptors PTCH and SMO. It inhibits the growth of primary pancreatic xenografts without non-specifically inhibiting pancreatic cell proliferation in vitro and has recently entered the clinic. It also inhibits ABCG2, Pgp, and MRP1-important ABC transporters associated with MDR. The IC50 values of GDC-0449 (Vismodegib) for inhibition of ABCG2 and Pgp were about1.4 and 3.0 ¦ÌM, respectively. It has been used to treat medulloblastoma in animal models.

prudect name : GDC-0449 (Vismodegib) is a more potent novel and specific synthetic oral hedgehog pathway inhibitor with an IC50 of 3 nM. It targets the Hedgehog signaling pathway, blocking…

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