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Page 1
Novel Janus-kinase (JAK) Inhibitors in Myelofibrosis.
Ipek Y, Kilic B, Gunay UB, Eskazan AE. Ipek Y, et al. Expert Opin Investig Drugs. 2023 Jul-Dec;32(10):931-940. doi: 10.1080/13543784.2023.2269078. Epub 2023 Nov 6. Expert Opin Investig Drugs. 2023. PMID: 37811861 Review.
AREAS COVERED: This review includes the current status of JAKi treatment for myelofibrosis, mainly focusing on investigational JAKis; jaktinib, lestaurtinib, itacitinib, gandotinib, BMS-911543, ilginatinib, TQ05105, and flonoltinib maleate. MEDLINE and clinicaltrial …
AREAS COVERED: This review includes the current status of JAKi treatment for myelofibrosis, mainly focusing on investigational JAKis; jaktin …
Characterization of BMS-911543, a functionally selective small-molecule inhibitor of JAK2.
Purandare AV, McDevitt TM, Wan H, You D, Penhallow B, Han X, Vuppugalla R, Zhang Y, Ruepp SU, Trainor GL, Lombardo L, Pedicord D, Gottardis MM, Ross-Macdonald P, de Silva H, Hosbach J, Emanuel SL, Blat Y, Fitzpatrick E, Taylor TL, McIntyre KW, Michaud E, Mulligan C, Lee FY, Woolfson A, Lasho TL, Pardanani A, Tefferi A, Lorenzi MV. Purandare AV, et al. Leukemia. 2012 Feb;26(2):280-8. doi: 10.1038/leu.2011.292. Epub 2011 Oct 21. Leukemia. 2012. PMID: 22015772
We report the characterization of BMS-911543, a potent and selective small-molecule inhibitor of the Janus kinase (JAK) family member, JAK2. ...Similar to these in vitro observations, BMS-911543 was also highly active in in vivo models of JAK2 signalin …
We report the characterization of BMS-911543, a potent and selective small-molecule inhibitor of the Janus kinase (JAK) family …
Single agent BMS-911543 Jak2 inhibitor has distinct inhibitory effects on STAT5 signaling in genetically engineered mice with pancreatic cancer.
Mace TA, Shakya R, Elnaggar O, Wilson K, Komar HM, Yang J, Pitarresi JR, Young GS, Ostrowski MC, Ludwig T, Bekaii-Saab T, Bloomston M, Lesinski GB. Mace TA, et al. Oncotarget. 2015 Dec 29;6(42):44509-22. doi: 10.18632/oncotarget.6332. Oncotarget. 2015. PMID: 26575024 Free PMC article.
In vivo administration of BMS-911543 significantly reduced pSTAT5 and FoxP3 positive cells within the pancreas, but did not alter STAT3 phosphorylation. ...Similarly, BMS-911543 had little in vitro effect on the viability of both murine and human PDAC- …
In vivo administration of BMS-911543 significantly reduced pSTAT5 and FoxP3 positive cells within the pancreas, but did not al …
Determinants of survival and retrospective comparisons of 183 clinical trial patients with myelofibrosis treated with momelotinib, ruxolitinib, fedratinib or BMS- 911543 JAK2 inhibitor.
Gangat N, Begna KH, Al-Kali A, Hogan W, Litzow M, Pardanani A, Tefferi A. Gangat N, et al. Blood Cancer J. 2023 Jan 4;13(1):3. doi: 10.1038/s41408-022-00780-9. Blood Cancer J. 2023. PMID: 36599841 Free PMC article.
Between October 2007 and July 2013, 183 Mayo Clinic patients (median age 65 years; 58% males) with high/intermediate risk myelofibrosis (MF) were enrolled in consecutive phase 1/2 JAK2 inhibitor (JAKi) clinical trials with momelotinib (n = 79), ruxolitinib (n = 50), fedratinib (n …
Between October 2007 and July 2013, 183 Mayo Clinic patients (median age 65 years; 58% males) with high/intermediate risk myelofibrosis (MF) …
Limited efficacy of BMS-911543 in a murine model of Janus kinase 2 V617F myeloproliferative neoplasm.
Pomicter AD, Eiring AM, Senina AV, Zabriskie MS, Marvin JE, Prchal JT, O'Hare T, Deininger MW. Pomicter AD, et al. Exp Hematol. 2015 Jul;43(7):537-45.e1-11. doi: 10.1016/j.exphem.2015.03.006. Epub 2015 Apr 24. Exp Hematol. 2015. PMID: 25912019 Free PMC article.
To explore the clinical potential of this inhibitor, we tested BMS-911543 in a murine retroviral transduction-transplantation model of JAK2(V617F) MPN. ...Inhibitor activity after dosing was confirmed in a cell culture assay using the plasma of dosed mice and phosph …
To explore the clinical potential of this inhibitor, we tested BMS-911543 in a murine retroviral transduction-transplantation …
C-H Arylation in the Formation of a Complex Pyrrolopyridine, the Commercial Synthesis of the Potent JAK2 Inhibitor, BMS-911543.
Fox RJ, Cuniere NL, Bakrania L, Wei C, Strotman NA, Hay M, Fanfair D, Regens C, Beutner GL, Lawler M, Lobben P, Soumeillant MC, Cohen B, Zhu K, Skliar D, Rosner T, Markwalter CE, Hsiao Y, Tran K, Eastgate MD. Fox RJ, et al. J Org Chem. 2019 Apr 19;84(8):4661-4669. doi: 10.1021/acs.joc.8b02383. Epub 2018 Nov 12. J Org Chem. 2019. PMID: 30388009
The development of an improved short and efficient commercial synthesis of the JAK2 inhibitor, a complex pyrrolopyridine, BMS-911543, is described. During the discovery and development of this synthesis, a Pd-catalyzed C-H functionalization was invented which enable …
The development of an improved short and efficient commercial synthesis of the JAK2 inhibitor, a complex pyrrolopyridine, BMS-9115 …
Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms.
Wan H, Schroeder GM, Hart AC, Inghrim J, Grebinski J, Tokarski JS, Lorenzi MV, You D, Mcdevitt T, Penhallow B, Vuppugalla R, Zhang Y, Gu X, Iyer R, Lombardo LJ, Trainor GL, Ruepp S, Lippy J, Blat Y, Sack JS, Khan JA, Stefanski K, Sleczka B, Mathur A, Sun JH, Wong MK, Wu DR, Li P, Gupta A, Arunachalam PN, Pragalathan B, Narayanan S, K C N, Kuppusamy P, Purandare AV. Wan H, et al. ACS Med Chem Lett. 2015 Jul 12;6(8):850-5. doi: 10.1021/acsmedchemlett.5b00226. eCollection 2015 Aug 13. ACS Med Chem Lett. 2015. PMID: 26288683 Free PMC article.
X-ray structure and ADME guided refinement of C-4 heterocycles to address metabolic liability present in dialkylthiazole 1 led to the discovery of a clinical candidate, BMS-911543 (11), with excellent kinome selectivity, in vivo PD activity, and safety profile....
X-ray structure and ADME guided refinement of C-4 heterocycles to address metabolic liability present in dialkylthiazole 1 led to the discov …
Ni-Catalyzed C-H Functionalization in the Formation of a Complex Heterocycle: Synthesis of the Potent JAK2 Inhibitor BMS-911543.
Fitzgerald MA, Soltani O, Wei C, Skliar D, Zheng B, Li J, Albrecht J, Schmidt M, Mahoney M, Fox RJ, Tran K, Zhu K, Eastgate MD. Fitzgerald MA, et al. J Org Chem. 2015 Jun 19;80(12):6001-11. doi: 10.1021/acs.joc.5b00572. Epub 2015 May 1. J Org Chem. 2015. PMID: 25848821
BMS-911543 is a complex pyrrolopyridine investigated as a potential treatment for myeloproliferative disorders. ...
BMS-911543 is a complex pyrrolopyridine investigated as a potential treatment for myeloproliferative disorders. ...
A UHPLC-MS/MS bioanalytical assay for the determination of BMS-911543, a JAK2 inhibitor, in human plasma.
Liu J, Yuan L, Liu G, Shen JX, Aubry AF, Arnold ME, Ji QC. Liu J, et al. J Chromatogr B Analyt Technol Biomed Life Sci. 2015 Jun 1;991:85-91. doi: 10.1016/j.jchromb.2015.04.013. Epub 2015 Apr 17. J Chromatogr B Analyt Technol Biomed Life Sci. 2015. PMID: 25930207
Chromatographic separation was achieved within 2min on a Zorbax Extend-C18 column with an isocratic elution. BMS-911543 and its internal standard were detected by positive ion electrospray tandem mass spectrometry. ...The assay has high recovery (80%) and minimal ma …
Chromatographic separation was achieved within 2min on a Zorbax Extend-C18 column with an isocratic elution. BMS-911543 and it …
16 results