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Avosentan(Ro 67-0565; SPP-301) is an Endothelin Antagonist.

June 21, 2017

prudect name : Avosentan(Ro 67-0565; SPP-301) is an Endothelin Antagonist.Avosentan; Ro 67-0565 SPP-301 Synonyms: Avosentan; Ro 67-0565 SPP-301CAS NO: 290815-26-8Molecular Formula: C23H21N5O5SMolecular Weight: 479.51Purity: 98% minSolubility: In DMSOStorage: -20°C 85622-93-1…

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N-[2-[[2-(Dimethylamino)ethyl]methylamino]-5-[[4-(1H-indol-3-yl)-2-pyrimidinyl]amino]-4-methoxyphenyl]-2-propenamide

prudect name : N-[2-[[2-(Dimethylamino)ethyl]methylamino]-5-[[4-(1H-indol-3-yl)-2-pyrimidinyl]amino]-4-methoxyphenyl]-2-propenamideAZ5104 Synonyms: CAS NO: 1421373-98-9Molecular Formula: C27H31N7O2Molecular Weight: 485.58Purity: 98% minSolubility: In DMSOStorage: -20°C 53179-13-8 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18499892

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AT13387 is a synthetic, orally bioavailable, small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity. Hsp90 inhibitor AT13387 selectively binds to Hsp90, thereby inhibiting its chaperone function and promoting the degradation of oncogenic signaling proteins involved in tumor cell proliferation and survival. Hsp90, a chaperone protein upregulated in a variety of tumor cells, regulates the folding, stability and degradation of many oncogenic signaling proteins.

prudect name : AT13387 is a synthetic, orally bioavailable, small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity. Hsp90 inhibitor AT13387 selectively binds to Hsp90, thereby inhibiting…

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A66 is a highly specific and selective p110¦Á inhibitor with IC50 of 32,30 and 43 nM for p110¦Á, p110¦Á/E545K, p110¦Á/H1047R, respectively. A66 S potently blocks phosphorylation of Akt/PKB in a subgroup of the cell lines tested demonstrates that some cell types are highly dependent on p110¦Á activity. A66 is more than 100 fold less active against the other class-I PI 3-kinase isoforms and had not inhibitory activity against 200 protein kinases when tested at 10 micromolar. This makes it the most selective and specific p110alpha inhibitor available for research purposes. A66 S is more efficacious at inducing growth delay in HCT116. While A66 S did not induce tumor regression in xenograft models the ability to induce growth delay indicates p110¦Á selective have to ability to be effective as cytostatic agents in some tumor types.

prudect name : A66 is a highly specific and selective p110¦Á inhibitor with IC50 of 32,30 and 43 nM for p110¦Á, p110¦Á/E545K, p110¦Á/H1047R, respectively. A66 S potently blocks phosphorylation of…

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ARRY-380 is equipotent against truncated p95-HER2 with an IC50 of 7 nM. [1] However, ARRY-380 suppresses EGFR with an IC50 of 4 ¦ÌM. ARRY-380 is about 500-fold selective for HER2 versus EGFR.ARRY-380 significantly prevents the growth of tumor in multiple HER2-dependent tumor xenograft models and displays additive activity in combination with standard-of-care agents.

prudect name : ARRY-380 is equipotent against truncated p95-HER2 with an IC50 of 7 nM. [1] However, ARRY-380 suppresses EGFR with an IC50 of 4 ¦ÌM. ARRY-380 is about 500-fold…

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Overexpression of the prosurvival Bcl-2 family members (Bcl-2,Bcl-xL,and Mcl-1) is commonly associated with tumor maintenance, progression, and chemoresistance. Binding affinities were determined with competitive fluorescence polarization assays and a time-resolved fluorescence resonance energy transfer assay (Ki¡¯s of <1 nmol/L for Bcl-2, Bcl-xL, and Bcl-w). The oral bioavailability of ABT-263 (Navitoclax) in preclinical animal models is 20% to 50%, depending on formulation.

prudect name : Overexpression of the prosurvival Bcl-2 family members (Bcl-2,Bcl-xL,and Mcl-1) is commonly associated with tumor maintenance, progression, and chemoresistance. Binding affinities were determined with competitive fluorescence polarization assays…

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Synonym: ACT-D || actinomycin C1 || actinomycin D || actinomycin I1 || actinomycin IV || actinomycin X 1 || actinomycin-[thr-val-pro-sar-meval] || AD || dactinomycine || meractinomycin || US brand names: Cosmegen || Lyovac Cosmegen || Abbreviation: DACT Chemical structure name: 2-bis[cyclo(N-methyl-L-valyl-sarcosyl-L-prolyl-D-valyl-L-threonyl)]-1,9 dimethyl-4,6 3H-phenoxazinone-3.

prudect name : Synonym: ACT-D || actinomycin C1 || actinomycin D || actinomycin I1 || actinomycin IV || actinomycin X 1 || actinomycin-[thr-val-pro-sar-meval] || AD || dactinomycine || meractinomycin ||…

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Axitinib exhibits primary inhibition to orthotopically transplanted models such as M24met (melanoma), HCT-116 (colorectal cancer), and SN12C (renal cell carcinoma). [1] Axitinib delays the tumor growth with 11.4 days compared to the controls (p.o. 30 mg/kg) and decreases the Mean Vessels Density (MVD) to 21, compared to 49 in controls, in IGR-N91 ﬂank xenografts. [2] Axitinib significantly inhibits growth and disrupts tumor microvasculature in BT474 breast cancer model at 10¨C100 mg/kg. [3] Axitinib has shown single-agent activity in variable tumors, including renal cell carcinoma, thyroid cancer, non-small cell lung cancer, and melanoma.

prudect name : Axitinib exhibits primary inhibition to orthotopically transplanted models such as M24met (melanoma), HCT-116 (colorectal cancer), and SN12C (renal cell carcinoma). [1] Axitinib delays the tumor growth with…

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AZD8186 potently inhibits p-Akt in MDA-MB-468 cells sensitive to PI3K¦Â inhibition and Jeko B cells sensitive to PI3K¦Ä inhibition with IC50 of 3 nM and 4 nM, respectively. AZD8186 shows preferred growth inhibition activity in most PTEN deficient cell lines with GI50 of <1 ¦ÌM.

prudect name : AZD8186 potently inhibits p-Akt in MDA-MB-468 cells sensitive to PI3K¦Â inhibition and Jeko B cells sensitive to PI3K¦Ä inhibition with IC50 of 3 nM and 4 nM,…

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Potent and selective tyrosine kinase (Trk) inhibitor with IC50 to 2 and 8 nM for TrkA and TrkB respectively; AZ-23 showed in vivo TrkA kinase inhibition and efficacy in mice following oral administration; having potential for therapeutic utility in neuroblastoma and multiple other cancer indications.

prudect name : Potent and selective tyrosine kinase (Trk) inhibitor with IC50 to 2 and 8 nM for TrkA and TrkB respectively; AZ-23 showed in vivo TrkA kinase inhibition and…

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