Bosutinib is a dual kinase inhibitor. With imatinib, bosutinib both Abl and inhibition of their own SRC kinase, thereby inhibiting cell growth and apoptosis (cell death)

June 21, 2017

prudect name : Bosutinib is a dual kinase inhibitor. With imatinib, bosutinib both Abl and inhibition of their own SRC kinase, thereby inhibiting cell growth and apoptosis (cell death)Bosutinib(SKI-606) Synonyms:…

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Brigatinib is a highly potent and selective investigational ALK inhibitor with mean IC50 value £¼ 100 nM in Ba/F3 cells. IC50 value: £¼ 100 nM Target: pan-ALK in vitro: Brigatinib inhibits all 17 ALK mutants previously observed to confer resistance to Crizotinib, Ceritinib, and/or Alectinib. in vivo: Brigatinib uniquely maintains substantial activity against the highly recalcitrant G1202R mutant. Brigatinib has exhibited promising antitumor activity in patients with Crizotinib-resistant disease in an ongoing phase 1/2 clinical trial.

prudect name : Brigatinib is a highly potent and selective investigational ALK inhibitor with mean IC50 value £¼ 100 nM in Ba/F3 cells. IC50 value: £¼ 100 nM Target: pan-ALK…

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BIBW2992 (Afatinib) is an irreversible EGFR/HER2 inhibitor with an IC50 of 14 nM for in vitro potency against HER2. In cell-free in vitro kinase assays, BIBW2992 shows potent activity against wild-type and mutant forms of EGFR and HER2, similar to gefitinib in potency for L858R EGFR, but about 100-fold more active against the gefitinib resistant L858R-T790M EGFR double mutant, with an IC50 of 10 nM. BIBW2992 was effective in inhibiting survival of lung cancer cell lines harboring wild-type (H1666) or L858R/T790M (NCI-H1975) EGFR, with IC50s below 100 nM for these isoforms resistant to first-generation inhibitors anda subnanomolar IC50 for the gefitinibsensitive L858R expressedby H3255. Assessed in a standard xenograft model of the epidermoid carcinoma cell line A431. Daily oral treatment with BIBW2992 at 20 mg/kg for 25 days resulted in dramatic tumor regression with a cumulative treated/control tumor volume ratio (T/C ratio) of 2%.

prudect name : BIBW2992 (Afatinib) is an irreversible EGFR/HER2 inhibitor with an IC50 of 14 nM for in vitro potency against HER2. In cell-free in vitro kinase assays, BIBW2992 shows…

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BRD73954 ia a potent and selective HDAC inhibitor with IC50 of 36 nM and 120 nM for HDAC6 and HDAC8, respectively.

prudect name : BRD73954 ia a potent and selective HDAC inhibitor with IC50 of 36 nM and 120 nM for HDAC6 and HDAC8, respectively.BRD73954 Synonyms: CAS NO: 1440209-96-0Molecular Formula: C16H16N2O3Molecular…

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Betamustine acts as an alkylating agent causing intra-strand and inter-strand cross-links between DNA bases. Bendamustine may differ from other alkylators in that it may be more potent in activating p53-dependent stress pathways and inducing apoptosis; it may induce mitotic catastrophe; and it may activate a base excision DNA repair pathway rather than an alkyltransferase DNA repair mechanism. Accordingly, this agent may be more efficacious and less susceptible to drug resistance than other alkylators.

prudect name : Betamustine acts as an alkylating agent causing intra-strand and inter-strand cross-links between DNA bases. Bendamustine may differ from other alkylators in that it may be more potent…

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prudect name : BMS-791325;BeclabuvirSynonyms: CAS NO: 958002-33-0 958002-36-3 (hydrochloride)Molecular Formula: C36H45N5O5SMolecular Weight: 659.838Purity: 98% minSolubility:

prudect name : BMS-791325;Beclabuvir Synonyms: CAS NO: 958002-33-0 958002-36-3 (hydrochloride)Molecular Formula: C36H45N5O5SMolecular Weight: 659.838Purity: 98% minSolubility: in DMSOStorage: -20oC Daporinad References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18505320

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BIBF1120 inhibits PDGFR kinase activity of PDGFR alpha and PDGFR beta types with IC50 values of 59 and 65 nM, respectively. In addition, BIBF1120 suppresses the FGFR subtypes with IC50 of 60, 37 and 108 nM for FGFR1, FGFR2, and FGFR3, respectively. BIBF1120 binds to the ATP-binding site in the cleft between the amino and carboxy terminal lobes of the kinase domain. The indolinone scaffold forms two hydrogen bonds with the backbone nitrogen of Cys919 and the backbone carbonyl oxygen of Glu917 in the hinge region. BIBF 1120 inhibits proliferation of PDGF-BB stimulated BRPs with an EC50 of 79 nM in cell assays. BIBF1120 at concentrations as low as 100 nM blocks activation of MAPK after stimulation with 5% serum plus PDGF-BB. In cultures of human vascular smooth muscle cells (HUASMC), BIBF1120 prevents PDGF-BB stimulated proliferation with an EC50 of 69 nM.

prudect name : BIBF1120 inhibits PDGFR kinase activity of PDGFR alpha and PDGFR beta types with IC50 values of 59 and 65 nM, respectively. In addition, BIBF1120 suppresses the FGFR…

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prudect name : BenzbromaroneSynonyms: CAS NO: 3562-84-3Molecular Formula: C17H12Br2O3Molecular Weight: 424.08Purity: 99%Solubility: Storage: −20°C

prudect name : Benzbromarone Synonyms: CAS NO: 3562-84-3Molecular Formula: C17H12Br2O3Molecular Weight: 424.08Purity: 99%Solubility: Storage: −20°C 2 years CJ-023423 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18505192

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Bicalutamide capsules for the treatment of advanced prostate cancer, anti-cancer drug

prudect name : Bicalutamide capsules for the treatment of advanced prostate cancer, anti-cancer drugBicalutamide Synonyms: CAS NO: 90357-06-5Molecular Formula: C18H14F4N2O4SMolecular Weight: 430.37Purity: 99%Solubility: Storage: −20°C 2 years Z-VAD(OMe)-FMK References PubMed…

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Batimastat (BB-94) is a potent, broad spectrum matrix metalloprotease (MMP) inhibitor for MMP-1, MMP-2, MMP-9, MMP-7 and MMP-3 with IC50 of 3 nM, 4 nM, 4 nM, 6 nM and 20 nM, respectively. Also inhibits the activitity of other metalloproteases, such as ADAM17.

prudect name : Batimastat (BB-94) is a potent, broad spectrum matrix metalloprotease (MMP) inhibitor for MMP-1, MMP-2, MMP-9, MMP-7 and MMP-3 with IC50 of 3 nM, 4 nM, 4 nM,…

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