CX-6258 is a pan-Pim kinases inhibitor with excellent biochemical potency and kinase selectivity. CX-6258 exhibited in vitro synergy with chemotherapeutics and robust in vivo efficacy in two Pim kinases driven tumor models. Inhibition of Pim kinases is expected to have a beneficial effect as cancer therapy.

 June 21, 2017

prudect name : CX-6258 is a pan-Pim kinases inhibitor with excellent biochemical potency and kinase selectivity. CX-6258 exhibited in vitro synergy with chemotherapeutics and robust in vivo efficacy in two…

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CAL-101 is a potent PI3K p110¦Ä inhibitor with an IC50 of 65 nM. CAL-101 blocked constitutive phosphatidylinositol-3-kinase signaling, resulting in decreased phosphorylation of Akt and other downstream effectors, an increase in poly(ADP-ribose) polymerase and caspase cleavage and an induction of apoptosis. CAL-101 has 40 to 300-fold selectivity compared to other PI3K isoforms. In vitro studies of 0.1 to 10 µM CAL-101 showed inhibition of pAKT expression and/or apoptotic effects against primary chronic lymphocytic leukemia (CLL) and acute myeloid leukemia (AML) cells and against a range of leukemia and lymphoma cell lines.

prudect name : CAL-101 is a potent PI3K p110¦Ä inhibitor with an IC50 of 65 nM. CAL-101 blocked constitutive phosphatidylinositol-3-kinase signaling, resulting in decreased phosphorylation of Akt and other downstream…

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Canagliflozin is a novel C-glucoside with thiophene ring. Canagliflozin inhibits Na+-dependent 14C-AMG uptake in a concentration-dependent fashion. Canagliflozin inhibits 14C-AMG uptake in CHO-hSGLT1 and mSGLT1 cells with IC50 of 0.7 ¦ÌM and >1 ¦ÌM, respectively. Canagliflozin inhibits the facilitative (non-Na+-linked) GLUT-mediated 2H-2-DG uptake in L6 myoblasts by less than 50%. In sham-injected oocytes, Canagliflozin (10 µM) or phlorizin (3 mM) alone in the presence of 50 µM DNJ does not affect currents. In SGLT3-injected oocytes, DMSO and Canagliflozin 10 µM inhibits DNJ-induced currents by 15.6% and 23.4%, respectively.

prudect name : Canagliflozin is a novel C-glucoside with thiophene ring. Canagliflozin inhibits Na+-dependent 14C-AMG uptake in a concentration-dependent fashion. Canagliflozin inhibits 14C-AMG uptake in CHO-hSGLT1 and mSGLT1 cells with…

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prudect name : Cidofovir hydrateSynonyms: CAS NO: 149394-66-1Molecular Formula: C8H14N3O6P.2(H2O)Molecular Weight: 315.22Purity: 98% minSolubility: In

prudect name : Cidofovir hydrate Synonyms: CAS NO: 149394-66-1Molecular Formula: C8H14N3O6P.2(H2O)Molecular Weight: 315.22Purity: 98% minSolubility: In DMSOStorage: -20¡æ MELK inhibitor References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18508602

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prudect name : CL-BKSynonyms: CAS NO: 178454-81-4Molecular Formula: Molecular Weight: Purity: 98% minSolubility: Storage: -20¡æ

prudect name : CL-BK Synonyms: CAS NO: 178454-81-4Molecular Formula: Molecular Weight: Purity: 98% minSolubility: Storage: -20¡æ Ataluren References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18508584

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CHIR-124 is a novel and potent chk1 inhibitor with an IC50 of 0.3 nM. Chk1 kinase is a critical regulator of both the S and G2/M phase cell cycle checkpoints in response to DNA damage. CHIR-124 has been shown that inhibitors of chk1 can selectively sensitize tumor cells with mutant p53 to genotoxic agents.

prudect name : CHIR-124 is a novel and potent chk1 inhibitor with an IC50 of 0.3 nM. Chk1 kinase is a critical regulator of both the S and G2/M phase…

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prudect name : Cefoselis sulfateSynonyms: CAS NO: 122841-12-7Molecular Formula: C19H22N8O6S2.H2O4S;C19H24N8O10S3Molecular Weight: 620.64Purity: 98% minSolubility: Storage:

prudect name : Cefoselis sulfate Synonyms: CAS NO: 122841-12-7Molecular Formula: C19H22N8O6S2.H2O4S;C19H24N8O10S3Molecular Weight: 620.64Purity: 98% minSolubility: Storage: −20°C LY411575 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18508551

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XL-184 free base (Cabozantinib) is a potent multitargeted VEGFR2, Met, FLT3, Tie2, Kit and Ret inhibitor with IC50 of 0.035, 1.8, 14.4, 14.3 and 4.6 nM for VEGFR2, Met, FLT3, Tie2 and Kit, respectively. In cells XL-184 free base (Cabozantinib) is also very potent, with IC50 under 10 nM for VEGFR2, MET, Kit and FLT3-ITD mechanistic assays. In in vitro angiogenesis assays, XL-184 free base (Cabozantinib) exhibits single-digit nanomolar potency. In mouse xenograft models, XL-184 free base (Cabozantinib), dosed orally, demonstrated dose-dependent inhibition of tumor growth and tumor regression, associated with disruption of the tumor vasculature and extensive tumor cell apoptosis.

prudect name : XL-184 free base (Cabozantinib) is a potent multitargeted VEGFR2, Met, FLT3, Tie2, Kit and Ret inhibitor with IC50 of 0.035, 1.8, 14.4, 14.3 and 4.6 nM for…

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Cyclopamine inhibits the hedgehog signaling pathway (Hh) by influencing the balance between the active and inactive forms of the Smoothened protein. The hedgehog signaling pathway carries out important functions in embryonic development and when it goes awry, deformities can occur. However, errant activation of the pathway can also trigger cancer in adult humans.

prudect name : Cyclopamine inhibits the hedgehog signaling pathway (Hh) by influencing the balance between the active and inactive forms of the Smoothened protein. The hedgehog signaling pathway carries out…

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prudect name : Cilastatin sodiumSynonyms: CAS NO: 81129-83-1Molecular Formula: C16H25N2NaO5SMolecular Weight: 380.43Purity: ≥99%Solubility: Storage: −20°C

prudect name : Cilastatin sodium Synonyms: CAS NO: 81129-83-1Molecular Formula: C16H25N2NaO5SMolecular Weight: 380.43Purity: ≥99%Solubility: Storage: −20°C 2 years LBH-589 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18508453

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