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Poly(adenosine diphosphate-ribose) polymerase (PARP) is anenzyme that is involved in a specific kind of DNA repair called base-excision repair, which is used when there is an error in a strand of the DNA.IC50 (¦ÌM):PARP-1= 0.005,PARP-2= 0.001 , PF50=25.8.AZD2281(Olaparib) at 400 mg twice daily is well tolerated and highly active. The toxicity that was seen in BRCA1/BRCA2 carriers was similar to the previously reported toxicity in noncarriers

June 21, 2017

prudect name : Poly(adenosine diphosphate-ribose) polymerase (PARP) is anenzyme that is involved in a specific kind of DNA repair called base-excision repair, which is used when there is an error…

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Abiraterone (CB-7598, CB7598, CB 7598) is a potent steroidal cytochrome P450 17alpha-hydroxylase-17,20-lyase (CYP17) inhibitor with an IC50 at 4 nM. Abiraterone (CB-7598, CB7598, CB 7598) is currently undergoing phase II clinical trials as a potential compound for the treatment of prostate cancer. In preclinical studies, abiraterone (CB-7598, CB7598, CB 7598) has demonstrated the ability to selectively inhibit the target enzyme, resulting in inhibition of testosterone production in both the adrenals and the testes. Clinical studies demonstrated that CYP17 blockade by abiraterone acetate is safe and has significant antitumor activity in CRPC (castration-resistant prostate cancer).

prudect name : Abiraterone (CB-7598, CB7598, CB 7598) is a potent steroidal cytochrome P450 17alpha-hydroxylase-17,20-lyase (CYP17) inhibitor with an IC50 at 4 nM. Abiraterone (CB-7598, CB7598, CB 7598) is currently…

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Biological Activity Allosteric modulator of IRE1¦Á. Inhibits IRE1¦Á autophosphorylation (IC50 = 280 nM) and activates IRE1¦Á RNase activity.

prudect name : Biological Activity Allosteric modulator of IRE1¦Á. Inhibits IRE1¦Á autophosphorylation (IC50 = 280 nM) and activates IRE1¦Á RNase activity.APY 29 Synonyms: CAS NO: 1216665-49-4Molecular Formula: C17H16N8Molecular Weight: 332.36Purity:…

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Aliskiren hemifumarate is a hemifumarate salt form of Aliskiren. Aliskiren is a direct renin inhibitor with an IC50 of 0.72 nM against renin. Renin is the first enzyme in the renin-angiotensin-aldosterone system which plays a role in blood pressure control. Renin cleaves angiotensinogen to angiotensin I, which is in turn converted by (ACE) to angiotensin II. Angiotensin II has both direct and indirect effects on blood pressure. It directly causes arterial smooth muscle to contract, leading to vasoconstriction and increased blood pressure. Angiotensin II also stimulates the production of aldosterone from the adrenal cortex, which causes the tubules of the kidneys to increase reabsorption of sodium, with water following thereby increasing plasma volume and blood pressure. Aliskiren binds to the S3bp binding pocket of renin, essential for its activity. Binding to this pocket prevents the conversion of angiotensinogen to angiotensin I. Aliskiren is also available as combination therapy with hydrochlorothiazide.

prudect name : Aliskiren hemifumarate is a hemifumarate salt form of Aliskiren. Aliskiren is a direct renin inhibitor with an IC50 of 0.72 nM against renin. Renin is the first enzyme…

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AP23848 is a potent Bcr-Abl inhibitor. In a murine model, AP23848 inhibited activation-loop mutant Kit phosphorylation and tumor growth.

prudect name : AP23848 is a potent Bcr-Abl inhibitor. In a murine model, AP23848 inhibited activation-loop mutant Kit phosphorylation and tumor growth.AP23848 PF-562771 Synonyms: CAS NO: 834894-21-2Molecular Formula: C30H38N5O2PMolecular Weight:…

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APD668 is a potent GPR119 agonist with EC50 of 2.7 nM and 33 nM for hGPR119 and ratGPR119 respectively.

prudect name : APD668 is a potent GPR119 agonist with EC50 of 2.7 nM and 33 nM for hGPR119 and ratGPR119 respectively.APD668 Synonyms: CAS NO: 832714-46-2Molecular Formula: C21H24FN5O5SMolecular Weight: 477.51Purity:…

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AZD7762 is a novel checkpoint kinase inhibitor with an IC50 of 5 and <10 nM for CHK1 and CHK2, respectively. It significantly prolonged the median time required for tumor volume doubling in response to gemcitabine and radiation. Together, findings suggest that G(2) checkpoint abrogation and homologous recombination repair inhibition both contribute to sensitization by Chk1 inhibition. Furthermore, they support the clinical use of AZD7762 in combination with gemcitabine and radiation for patients with locally advanced pancreatic cancer.

prudect name : AZD7762 is a novel checkpoint kinase inhibitor with an IC50 of 5 and

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prudect name : Ametantrone(NSC 196473)Synonyms: CAS NO: 64862-96-0Molecular Formula: C26H36N4O8Molecular Weight: 532.59Purity: 98% minSolubility: in

prudect name : Ametantrone(NSC 196473) Synonyms: CAS NO: 64862-96-0Molecular Formula: C26H36N4O8Molecular Weight: 532.59Purity: 98% minSolubility: in DMSOStorage: -20oC 1243244-14-5 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18496773

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Abiraterone Acetate (CB 7630) is a highly active and selective 17¦Á-hydroxylase/17,20 lyase (CYP17A1) inhibitor with an IC50 of 72 nM. Abiraterone Acetate (CB 7630) inhibitor CYP11B1, CYP11B2 and CYP3A4 with IC50 of 1.6, 1.8 and 2.7 ¦ÌM. Abiraterone Acetate (CB 7630) is used in the study of castration-resistant prostate cancer. Abiraterone Acetate (CB 7630) blocks the formation of testosterone by inhibiting CYP17A1. Abiraterone Acetate (CB 7630) caused significant reductions in the weights of the ventral prostate and seminal vesicles. There was no reduction seen in the weight of these organs with KC. Abiraterone Acetate (CB 7630) reduced plasma testosterone to 0.1 nM or less, despite a three- to four-fold increase in the plasma level of luteinizing hormone (LH).

prudect name : Abiraterone Acetate (CB 7630) is a highly active and selective 17¦Á-hydroxylase/17,20 lyase (CYP17A1) inhibitor with an IC50 of 72 nM. Abiraterone Acetate (CB 7630) inhibitor CYP11B1, CYP11B2…

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AG-490 is a tyrosine kinase inhibitor of JAK2, EGFR, and Neu that belongs to the family of tyrphostins. In acute lymphoblastic leukemia studies the compound has been reported to inhibit JAK2 from B cell precursors. Additionally, AG-490 has been observed to block cytokine-induced activation of JAK2 in eosinophils and STAT3 activation in T cell lymphoma cells. Unlike other kinase inhibitors, AG-490 does not inhibit JAK1, Lck, Btk, Tyk2, Syk, Lyn, and Src. Research indicates that AG-490 inhibits IL-7 mediated proliferation. Inhibition of Jak kinase activity by AG-490 leads to lower levels of p85 phosphorylation and p-13 kinase activation. AG-490 is an inhibitor of JAK3.

prudect name : AG-490 is a tyrosine kinase inhibitor of JAK2, EGFR, and Neu that belongs to the family of tyrphostins. In acute lymphoblastic leukemia studies the compound has been…

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