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151386-42-4

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151386-42-4 Usage

Check Digit Verification of cas no

The CAS Registry Mumber 151386-42-4 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,5,1,3,8 and 6 respectively; the second part has 2 digits, 4 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 151386-42:
(8*1)+(7*5)+(6*1)+(5*3)+(4*8)+(3*6)+(2*4)+(1*2)=124
124 % 10 = 4
So 151386-42-4 is a valid CAS Registry Number.

151386-42-4Relevant articles and documents

Discovery, Optimization, and in Vivo Evaluation of Benzimidazole Derivatives AM-8508 and AM-9635 as Potent and Selective PI3Kδ Inhibitors

Shin, Youngsook,Suchomel, Julia,Cardozo, Mario,Duquette, Jason,He, Xiao,Henne, Kirk,Hu, Yi-Ling,Kelly, Ron C.,McCarter, John,McGee, Lawrence R.,Medina, Julio C.,Metz, Daniela,San Miguel, Tisha,Mohn, Deanna,Tran, Thuy,Vissinga, Christine,Wong, Simon,Wannberg, Sharon,Whittington, Douglas A.,Whoriskey, John,Yu, Gang,Zalameda, Leeanne,Zhang, Xuxia,Cushing, Timothy D.

, p. 431 - 447 (2016/01/28)

Lead optimization efforts resulted in the discovery of two potent, selective, and orally bioavailable PI3Kδ inhibitors, 1 (AM-8508) and 2 (AM-9635), with good pharmacokinetic properties. The compounds inhibit B cell receptor (BCR)-mediated AKT phosphorylation (pAKT) in PI3Kδ-dependent in vitro cell based assays. These compounds which share a benzimidazole bicycle are effective when administered in vivo at unbound concentrations consistent with their in vitro cell potency as a consequence of improved unbound drug concentration with lower unbound clearance. Furthermore, the compounds demonstrated efficacy in a Keyhole Limpet Hemocyanin (KLH) study in rats, where the blockade of PI3Kδ activity by inbibitors 1 and 2 led to effective inhibition of antigen-specific IgG and IgM formation after immunization with KLH.

HETEROCYCLIC COMPOUNDS AND THEIR USES

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Page/Page column 27, (2011/10/13)

Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.

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