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CDK9 Inhibitor

Poster

The CDK9 Inhibitor, Alvocidib, Potentiates the Non-Clinical Activity of Azacytidine or Decitabine in an MCL-1-Dependent Fashion, Supporting Clinical Exploration of a Decitabine and Alvocidib Combination

Kim W, Whatcott C, Siddiqui-Jain A, Anthony S, Bearss DJ, Warner SL (See Poster PDF)

60th American Society of Hematology Annual Meeting and Exposition; December 1-4, 2018; San Diego, CA

CDK9 Inhibitor

Poster

The Oral CDK9 Inhibitor, TP-1287, Is Active in Non-Clinical Models of Multiple Myeloma

Tyagi E, Whatcott C, Foulks JM, Siddiqui-Jain A, Bearss DJ, Warner SL (See Poster PDF)

60th American Society of Hematology Annual Meeting and Exposition; December 1-4, 2018; San Diego, CA

AXL Inhibitor

Poster

Evaluation of the Pharmacology, Pharmacodynamic Activity and Immune Response Modulation of the AXL Kinase Inhibitor TP-0903

Anthony SP, Sarantopoulos J, Beg MS, et al (See Poster PDF)

30th EORTC-NCI-AACR Symposium; November 13-16, 2018; Dublin, Ireland

ACVR1 Inhibitor

AXL Inhibitor

CDK9 Inhibitor

Poster

Phase II study incorporating a novel BH3-profiling biomarker approach of alvocidib followed by cytarabine and mitoxantrone in relapsed/refractory acute myeloid leukemia (AML)

Zeidner JF, Vigil CE, Lin T, et al

European Hematology Association 23rd Annual Congress; June 14-17, 2018; Stockholm, Sweden

ACVR1 Inhibitor

AXL Inhibitor

CDK9 Inhibitor

Poster

A phase 1a/1b first-in-human, open-label, dose-escalation, safety, pharmacokinetic, and pharmacodynamic study of oral TP-0903, a potent inhibitor of AXL kinase administered daily for 21 days

Sarantopoulos J, Beg MS, Fotopoulos G, et al

2018 American Society of Clinical Oncology Annual Meeting; June 1-5, 2018; Chicago, IL

CDK9 Inhibitor

PIM Inhibitor

Poster

Targeting Myc in triple-negative breast cancer models through the dual inhibition of PIM kinases and CDK9

Haws H, Kim W, Siddiqui-Jain A, Bearss DJ, Warner SL, Whatcott CJ

2017 AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics; October 26-30, 2017; Philadelphia, PA.

CDK9 Inhibitor

Targeting MCL-1–dependent cancers by CDK9 inhibition

Bearss DJ

Paper presented at: 9th International Conference on Leukemia and Hematologic Oncology; October 5-6, 2017; London, UK.

ACVR1 Inhibitor

AXL Inhibitor

PIM Inhibitor

Targeting novel kinases in hematologic malignancies

Warner SL

Paper presented at: 9th International Conference on Leukemia and Hematologic Oncology; October 5-6, 2017; London, UK

CDK9 Inhibitor

Poster

Alvocidib synergizes with venetoclax in preclinical models of multiple myeloma

Haws H, Livingston M, Kim W, et al

European Hematology Association 22nd Annual Congress; June 22-25, 2017; Madrid, Spain

CDK9 Inhibitor

Poster

Alvocidib synergizes with cytarabine and daunorubicin (7+3) in preclinical models of acute myeloid leukemia

Kim W, Haws H, Mangelson R, et al

European Hematology Association 22nd Annual Congress; June 22-25, 2017; Madrid, Spain

CDK9 Inhibitor

Poster

By an MCL-1–dependent mechanism, alvocidib potentiates the activity of cytarabine and mitoxantrone when administered in a time sequential regimen in AML

Haws H, Livingston M, Kim W, et al

European Hematology Association 22nd Annual Congress; June 22-25, 2017; Madrid, Spain

AXL Inhibitor

Poster

TP-0903, a novel Axl inhibitor with activity in drug resistant FLT3-ITD+ AML through a mechanism that includes FLT3 inhibition

Jeon JY, Park I-K, Buelow DR, et al

Blood. 2017;130(suppl 1):2522.

ACVR1 Inhibitor

Poster

TP-0184 inhibits ALK2/ACVR1, decreases hepcidin levels, and demonstrates activity in preclinical mouse models of functional iron deficiency

Peterson P, Kim W, Whatcott C, et al

Blood. 2017;130(suppl 1):937.

CDK9 Inhibitor

Poster

TP-1287, an oral prodrug of the cyclin-dependent kinase-9 inhibitor alvocidib

Kim W, Haws H, Peterson P, et al

American Association for Cancer Research Annual Meeting; April 1-5, 2017; Washington, DC

CDK9 Inhibitor

Poster

Alvocidib potentiates the activity of venetoclax in preclinical models of acute myeloid leukemia

Whatcott CJ, Bogenberger JM, Kim W, et al

58th American Society of Hematology Annual Meeting and Exposition; December 3-6, 2016; San Diego, CA

CDK9 Inhibitor

Sequential treatment of AML patients with alvocidib followed by cytarabine and mitoxantrone is highly effective through a mechanism dependent on MCL1 expression and function

Bearss DJ

Paper presented at: International Conference on Leukemia and Hematologic Oncology; October 17-18, 2016; Rome, Italy

CDK9 Inhibitor

Poster

Alvocidib potentiates the activity of ABT-199 in nonclinical models of acute myeloid leukemia

Whatcott C, Bogenberger J, Kim W, et al

European Hematology Association 21st Annual Congress; June 9-12, 2016; Copenhagen, Denmark

CDK9 Inhibitor

Poster

TP-1287, an oral prodrug of the cyclin-dependent kinase-9 inhibitor alvocidib

Kim W, Soh S, Lee YS, et al

European Hematology Association 21st Annual Congress; June 9-12, 2016; Copenhagen, Denmark

CDK9 Inhibitor

Poster

Targeting MCL-1 expression, through the inhibition of CDK9 and super enhancer driven transcription, offers multiple opportunities for rational drug combinations

Kim W, Soh KK, Lee YS, et al

American Association for Cancer Research Annual Meeting; April 16-20, 2016; New Orleans, LA

AXL Inhibitor

Poster

AXL inhibition leads to a reversal of a mesenchymal phenotype sensitizing cancer cells to targeted agents and immuno-oncology therapies

Soh KK, Kim W, Lee YS, et al

American Association for Cancer Research Annual Meeting; April 16-20, 2016; New Orleans, LA

ACVR1 Inhibitor

The ALK-2 inhibitor, TP-0184, demonstrates high distribution to the liver contributing to significant preclinical efficacy in mouse models of anemia of chronic disease

Peterson P, Kim W, Haws H, et al

Blood. 2016;128(22):263

CDK9 Inhibitor

Poster

Alvocidib potentiates the activity of cytarabine and mitoxantrone through the targeting of MCL-1 when administered in a time sequential regimen in AML

Kim W, Bahr BL, Soh KK, et al

57th American Society of Hematology Annual Meeting; December 5-8, 2015; Orlando, FL

AXL Inhibitor

Poster

Inhibition of Axl kinase reverses the mesenchymal phenotype in leukemic cells through the disruption of retinoid acid signaling

Soh KK, Bahr BL, Bearss JJ, et al

57th American Society of Hematology Annual Meeting; December 5-8, 2015; Orlando, FL

CDK9 Inhibitor

Poster

Alvocidib potentiates the activity of azacytidine in an MCL-1–dependent fashion

Kim W, Soh KK, Bearss JJ, et al

57th American Society of Hematology Annual Meeting; December 5-8, 2015; Orlando, FL

CDK9 Inhibitor

Poster

Mitochondrial profiling in AML patients treated with an alvocidib containing regimen reveals MCL1 dependency in responder bone marrow

Dettman EJ, Warner SL, Doykan C, et al

American Association for Cancer Research Annual Meeting; April 18-22, 2015; Philadelphia, PA

CDK9 Inhibitor

Poster

Combination strategies to target super enhancer transcriptional activity by CDK9 and BRD4 inhibition in acute myeloid leukemia

Bahr BL, Maughan KS, Soh KK, et al

American Association for Cancer Research Annual Meeting; April 18-22, 2015; Philadelphia, PA

PIM Inhibitor

Poster

Targeting the PIM kinases in combination with BTK inhibition is synergistic in preclinical models of B-cell malignancies

Bearss JJ, Bahr BL, Soh KK, et al

American Association for Cancer Research Annual Meeting; April 18-22, 2015; Philadelphia, PA

ACVR1 Inhibitor

Poster

Targeting cancer-induced anemia with hepcidin lowering ALK2 inhibitors

Peterson P, Kim W, Bearss JJ, et al

American Association for Cancer Research Annual Meeting; April 18-22, 2015; Philadelphia, PA

PIM Inhibitor

Poster

The use of kinome profiling to determine potential resistance pathways in pancreatic cancer cells treated with PIM kinase inhibitors

Singh V, Nixon B, Gilbert TSK, et al

American Association for Cancer Research Annual Meeting; April 18-22, 2015; Philadelphia, PA

ACVR1 Inhibitor

ALK2 inhibition via TP-0184 abrogates inflammation-induced hepcidin expression and is a potential therapeutic for anemia of chronic disease

Peterson P, Soh KK, Lee YS, et al

Blood. 2015;126(23):273.

AXL Inhibitor

Inhibition of Axl kinase reverses the mesenchymal phenotype in leukemia cells through the disruption of retinoic acid signaling

Soh KK, Bahr BL, Bearss JJ, et al

Blood. 2015;126(23):3253

CDK9 Inhibitor

Bcl-xL dependence predicts response to alvocidib in chronic lymphocytic leukemia patients [AACR abstract 907]

Pierceall WE, Warner SL, Lena RJ, et al

Cancer Res. 2014;74(19)(suppl):907

AXL Inhibitor

Inhibition of the tyrosine kinase receptor Axl blocks cell invasion and promotes apoptosis in pancreatic cancer cells [AACR abstract 5543]

Anderson M, Ober A, Mollard A, et al

Cancer Res. 2013;73(8)(suppl):5543

AXL Inhibitor

An epithelial-mesenchymal transition (EMT) gene signature to predict resistance to EGFR inhibition and AXL identification as a therapeutic target in head and neck squamous cell carcinoma [ASCO abstract 6011]

Cardnell R, Diao L, Wang J, et al

J Clin Oncol. 2013;31(15)(suppl):6011

PIM Inhibitor

Small molecule inhibitors of PIM kinases as potential treatments for urothelial carcinomas [AACR abstract 2174]

Carpenter KJ, Brog R, Moreno C, et al

Cancer Res. 2013;73(8)(suppl):2174

PIM Inhibitor

Proviral integration site Moloney murine leukemia virus (PIM) expression in urothelial carcinoma [abstract 791]

Albertson DJ, Bearss JJ, Bearss DJ, Tripp S, Liu T

Paper presented at: 102nd Annual Meeting of United States and Canadian Academy of Pathology (USCAP); March 2-8, 2013; Baltimore, MD

AXL Inhibitor

Targeting the Axl tyrosine kinase receptor in pancreatic cancer [AACR abstract 2577]

Call LT, Mollard A, Wade ML, et al

Cancer Res. 2011;71(8)(suppl):2577

AXL Inhibitor

Homology structure-based design, synthesis and biological evaluation of a series of novel Axl and Mer kinase inhibitors [AACR abstract 3609]

Mollard A, Warner SL, Call L, et al

Cancer Res. 2011;71(8)(suppl):3609

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