TG101348
TG101348 (SAR302503) is an orally available inhibitor of Janus kinase 2 (JAK-2) developed for the treatment of patients with myeloproliferative diseases including myelofibrosis. TG101348 acts as a competitive inhibitor of protein kinase JAK-2 with IC50=6 nM; related kinases FLT3 and RET are also sensitive, with IC50=25 nM and IC50=17 nM, respectively. Significantly less activity was observed against other tyrosine kinases including JAK3 (IC50=169 nM). In treated cells the inhibitor blocks downstream cellular signalling (JAK-STAT) leading to suppression of proliferation and induction of apoptosis.
Myelofibrosis is a myeloid malignancy associated with anemia, splenomegaly, and constitutional symptoms. Patients with myelofibrosis frequently harbor JAK-STAT activating mutations that are sensitive to TG101348. Phase I trial results focused on safety and efficacy of TG101348 in patients with high- or intermediate-risk primary or post–polycythemia vera/essential thrombocythemia myelofibrosis have been published in 2011.
Compound was originally discovered TargeGen then acquired by Sanofi-Aventis who continues its development under the code SAR302503.

This is an excerpt from the article TG101348 from the Wikipedia free encyclopedia. A list of authors is available at Wikipedia.
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SAR302503 (TG101348) JAK2 Inhibitor - Sanofi Oncology
SAR302503 (TG101348) is an oral, selective JAK2 inhibitor that is currently being investigated in a phase I trial in patients with myelofibrosis.
www.sanofioncology.com/pipeline/SAR302503.aspx
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TG101348 (SAR302503) | JAK Inhibitors |…
TG-101348 (SAR302503) is a selective inhibitor of JAK2 with IC50 of 3 nM, 35- and 334-fold more selective for JAK2 versus JAK1 and JAK3. Phase 1/2.Quality confirmed ...
www.selleckchem.com/products/tg-101348.html
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TG101348 - Wikipedia, the free encyclopedia
TG101348 (SAR302503) is an orally available inhibitor of Janus kinase 2 (JAK-2) developed for the treatment of patients with myeloproliferative diseases ...
en.wikipedia.org/wiki/TG101348
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Safety and efficacy of TG101348, a selective JAK2 inhibitor, in ...
Jan 10, 2011 ... Patients frequently harbor JAK-STAT activating mutations that are sensitive to TG101348, a selective small-molecule Janus kinase 2 (JAK2) ...
www.ncbi.nlm.nih.gov/pubmed/21220608
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Efficacy of TG101348, a selective JAK2 inhibitor, in treatment of a ...
We report that TG101348, a selective small-molecule inhibitor of JAK2 with an in vitro IC50 of approximately 3 nM, shows therapeutic efficacy in a murine model ...
www.ncbi.nlm.nih.gov/pubmed/18394554
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TG101348 | CAS 936091-26-8 | Santa Cruz Biotech
Buy TG101348 (CAS 936091-26-8), a selective inhibitor of JAK2, from Santa Cruz Biotechnology. Molecular Formula: C27H36N6O3S, Molecular Weight: ...
www.scbt.com/datasheet-364740-tg101348.html
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Safety and Efficacy of TG101348, a Selective JAK2 Inhibitor, in ...
Jan 10, 2011 ... In a multicenter phase I trial, oral TG101348 was administered once a ... cycles; the median cumulative exposure to TG101348 was 380 days.
jco.ascopubs.org/content/early/2011/01/10/JCO.2010.32.8021.full.pdf
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TG101348 | CAS # 936091-26-8 | BioVision Inc.
TG101348 is a potent, and selective inhibitor of JAK2 (IC₅₀ = 3 nM). It has a 35- and 334-fold selectivity over JAK3 and JAK1, respectively. | Product Name: ...
www.biovision.com/tg101348-6693.html
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Cancer Cell - Efficacy of TG101348, a Selective JAK2 Inhibitor, in ...
Apr 8, 2008 ... Efficacy of TG101348, a Selective JAK2 Inhibitor, in Treatment of a Murine Model of JAK2V617F-Induced Polycythemia Vera. Cancer Cell ...
www.cell.com/cancer-cell/abstract/S1535-6108(08)00045-7
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TG101348 | CAS#936091-26-8 | MedKoo Biosciences
General activitiy: TG101348 (SAR302503) was developed for the treatment of patients with myeloproliferative diseases including myelofibrosis. TG101348 acts  ...
www.medkoo.com/Anticancer-trials/TG101348.htm
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TG101348 in science
Full Text - Journal of Clinical Oncology
Mar 1, 2011 ... Patients and Methods In a multicenter phase I trial, oral TG101348 was ..... Debra Harris Nolan, Kristen Rice, and Tristan Loucks (University of ...
[PDF]Safety and Efficacy of TG101348, a Selective JAK2 Inhibitor, in ...
Jan 10, 2011 ... Stanford University School of Medicine,. Stanford, CA ... In a multicenter phase I trial, oral TG101348 was administered once a day to patients.
Safety and Efficacy of TG101348, a Selective JAK2 Inhibitor, in ...
Mar 1, 2011 ... Patients frequently harbor JAK-STAT activating mutations that are sensitive to TG101348, a selective small-molecule Janus kinase 2 (JAK2) ...
Paper: Efficacy and Safety Of Fedratinib (SAR302503/TG101348) In ...
661 Efficacy and Safety Of Fedratinib (SAR302503/TG101348) In Patients With ... 2Department of Hematology, Radboud University Medical Centre, Nijmegen, ...
Paper: A Phase I Evaluation of TG101348, a Selective JAK2 Inhibitor ...
Dec 3, 2009 ... 3Department of Medicine and Moores Cancer Center, University of California San ... Background: TG101348 is a potent, orally bioavailable, ...
Safety and efficacy of TG101348, a selective JAK2 ... - Faculty of 1000
Oct 1, 2009 ... This agent TG101348 was the second major JAK2. ... The University of Chicago Pritzker School of Medicine, Chicago, IL, USA. Follow. Photo of ...
A Dose-escalation Study of the Safety and Tolerability of Orally ...
... tolerability of orally administered TG101348 in patients with myelofibrosis. ... Stanford University School of Medicine 300 Pasteur Drive Stanford, CA 94305.
Specificity and mechanism-of-action of the JAK2 tyrosine kinase ...
... of the JAK2 tyrosine kinase inhibitors ruxolitinib and SAR302503 (TG101348).. ... Department of Biochemistry, University of Zürich, Switzerland. Leukemia: ...
Recent letters - Blood
Effective of the selective JAK2 inhibitor, TG101348 on dendritic cell function ... Princess Margaret Cancer Centre, University of Toronto, Toronto, Canada.
TargeGen Selects Jak2 Inhibitor Lead (TG101348) For Clinical ...
Jan 6, 2007 ... TargeGen, Inc., a biopharmaceutical company developing small molecule kinase inhibitor drugs, today announced that TG101348, an ...
Books on the term TG101348
Myeloproliferative Neoplasms: Biology and Therapy
Myeloproliferative Neoplasms: Biology and Therapy
Srdan Verstovsek, Ayalew Tefferi, 2010
Development of SB1518 will continue with the dose of 400 mg once daily recommended for the phase 2 trial. TG101348 TG101348 is a selective JAK2 inhibitor with IC50 values of 3 nM, having less potency against JAK3 (335× less potent) ...
Targeting Protein Kinases for Cancer Therapy
Targeting Protein Kinases for Cancer Therapy
David J. Matthews, 2010
An expert guide to targeting protein kinases in cancer therapyResearch has shown that protein kinases can instigate the formation and spread of cancer when they transmit faulty signals inside cells. Because of this fact, pharmaceutical scientists have targeted kinases for intensive study, and have been working to develop medicinal roadblocks to sev...
Myeloproliferative Neoplasms: Critical Concepts and Management
Myeloproliferative Neoplasms: Critical Concepts and Management
Tiziano Barbui, Ayalew Tefferi, 2012
The study has recently started, with an estimated enrolment of 300 patients. Results are expected in 2013. 18.2.2.3 TG101348 TG101348 is an orally available, selective JAK2 inhibitor. TG101348 has selective activity against JAK2 (IC50 = 3 ...
Annual Reports in Medicinal Chemistry, Volume 45
Annual Reports in Medicinal Chemistry, Volume 45
2010
Annual Reports in Medicinal Chemistry provides timely and critical reviews of important topics in medicinal chemistry together with an emphasis on emerging topics in the biological sciences, which are expected to provide the basis for entirely new future therapies. * Covers findings related to cardiovascular, inflammation, and pulmonary diseases* E...
Targeting Protein Kinases for Cancer Therapy
Targeting Protein Kinases for Cancer Therapy
David J. Matthews, Mary E. Gerritsen, 2011
TG101348. TG101348 (Figure 8.2)is an orallyavailable, potent,and selective inhibitor of JAK2, FLT3,and RET. Invitro, TG101348 exhibits potent inhibitory activity against JAK2 (IC 50 = 3 nM), FLT3 (15 nM),
Myeloproliferative Neoplasms: Biology and Therapy (Contemporary Hematology)
Myeloproliferative Neoplasms: Biology and Therapy (Contemporary Hematology)
2010
This succinct resource provides an ideal balance of the biology and practical therapeutic strategies for classic and non-classic BCR-ABL-negative myeloproliferative neoplasms. Utilizing current World Health Organization nomenclature, classification, and diagnostic criteria, international experts have assembled to convey the most up-to-date knowledg...
Cancer: New Insights for the Healthcare Professional: 2012 ...
Cancer: New Insights for the Healthcare Professional: 2012 ...
2012
We demonstrate that selective JAK2 inhibition by TG101348 during initial encounters between human T cells and allogeneic monocyte-derived dendritic cells induces durable, profound, and specific T-cell tolerance upon reexposure to the ...
Leukemia (Emerging Cancer Therapeutics V2 I2)
Leukemia (Emerging Cancer Therapeutics V2 I2)
2011
This issue of Emerging Cancer Therapeutics provides a comprehensive review for practitioners on the current status of leukemia treatment. Leukemia treatment has undergone major change over the course of the past few years and Leukemia addresses current best practices in the light of the most recent evidence. All of the chapters are written by inter...
Diagnostic Molecular Pathology in Practice: A Case-Based ...
Diagnostic Molecular Pathology in Practice: A Case-Based ...
Iris Schrijver, 2011
This patient was enrolled into a Phase II clinical trial of the JAK2-specific inhibitor TG101348 (TargeGen) [19]. During the course of therapy, she has been monitored with physical examinations and complete blood counts every four weeks, and ...
Myeloproliferative Neoplasms: Critical Concepts and Management (Hematologic Malignancies)
Myeloproliferative Neoplasms: Critical Concepts and Management (Hematologic Malignancies)
2012
This book focuses on three of the main categories of myeloproliferative neoplasm: polycythemia vera, essential thrombocythemia, and primary myelofibrosis. Relevant laboratory and clinical advances are comprehensively covered, and great emphasis is placed on the practical issues that challenge physicians in their daily practice. The main topics cons...
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TG101348
TG101348 (SAR302503) | JAK Inhibitors | Read Reviews & Product Citations
TG-101348 (SAR302503) is a selective inhibitor of JAK2 with IC50 of 3 nM, 35- and 334-fold more selective for JAK2 versus JAK1 and JAK3. Phase 1/2.Quality confirmed by NMR & HPLC. See customer reviews, validations & product citations.
www.selleckchem.com/products/tg-101348.html
TG101348 | Karebay
TG101348 is a selective small-molecule inhibitor of JAK2. The IC50 of TG101348 is 3 nM against JAK2. TG101348 also inhibits JAK2V617F with an IC50 of 3 nM. In contrast, TG101348 prevents Flt3 and Ret with IC50 of 15 and 48 nM, respectively. TG101348 has an IC50∼300-fold higher for the closely related JAK3. TG101348 is a less potent inhibitor of the JAK1 and TYK2 family members. TG101348 inhibits proliferation of both of a human erythroblast leukemia (HEL) cell line that harbors the JAK2V617F mutation and a murine pro-B cell line expressing human JAK2V617F (Ba/F3 JAK2V617F) The IC50 of TG101348 is 300 nM for either line.[1] TG10134 inhibits the growth of KITD816V-dependent mast cell leukemia cells by blocking JAK-STAT signaling.[2] TG101348 is well tolerated and produces significant reduction in disease burden of myelofibrosis.[3] TG101348 prevents the cytokine-independent growth of human erythroleukemia and Ba/F3-JAK2V617F cells with IC50 of 0.3 and 0.58 µM, respectively. TG101348 inhibits Ba/F3-MPLW515L cells with an IC50 of 0.62 µM. TG101348 significantly decreases the size of erythroid colonies (erythroid burst-forming unit) obtained from PV progenitor cells.[4]
www.karebaybio.com/products/tg101348-15152.html
TG101348 was synthesized through the Memorial Sloan-Kettering Can | microrna 1
Posted on October 28, 2013 by micr1251.
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Gerlinde Wernig & Gary Gilliland effectiveness of TG 101348 propecia 1mg purchase. » Making this world better
- Gerlinde Wernig & Gary Gilliland – effectiveness of TG 101348, a selective JAK2 inhibitor, In preclinical modelshe treatment of a mouse model of JAK2V617F Induced polycythemia vera, Session Type propecia 1mg purchase . TargeGen initiated operations in 2002 and increased capital from top-tier venture capital sources.
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TG101348 was synthesized by the Memorial Sloan-Kettering Cancer C | Peptides Price
Posted on October 28, 2013 by admin.
peptidesprice.com/tg101348-was-synthesized-by-the-memorial-sloan-kettering-cancer-c
All graphs had been gexamined by XTT in the presence of TG101348 | inhibitor library
Posted on October 28, 2013 by admin.
inhibitorlibrary.com/all-graphs-had-been-gexamined-by-xtt-in-the-presence-of-tg101348
All graphs have been gexamined by XTT in the presence of TG101348 | checkpoint inhibitor
Posted on October 28, 2013 by chec5322.
checkpointinhibitor.com/all-graphs-have-been-gexamined-by-xtt-in-the-presence-of-tg101348
TargeGen Announces Successful Completion of Clinical Trial of JAK2 Inhibitor TG101348 in Myelofibrosis Patients - Drugs.com MedNews
TargeGen, Inc. today announced that the Company has successfully completed a 59 patient, multicenter clinical trial of TG101348, an oral, potent, and highly sel
www.drugs.com/clinical_trials/targegen-announces-successful-completion-clinical-trial-jak2-inhibitor-tg101348-myelofibrosis-8292.html
TargeGen Initiates Trial Of JAK2 Inhibitor TG101348 In Myeloproliferative Disease Patients
TargeGen has started a multi-center Phase I/II clinical trial of TG101348, an oral, potent, and highly selective inhibitor of JAK2 in patients with myeloproliferative diseases.
www.emaxhealth.com/95/20594.html
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