Initial testing (stage 1) of BAL101553, a novel tubulin binding agent, by the pediatric preclinical testing program

E. Anders Kolb; Richard Gorlick; Stephen T. Keir; John M. Maris; Min H. Kang; C. Patrick Reynolds; Richard B. Lock; Hernan Carol; Jianrong Wu; Raushan T. Kurmasheva; Peter J. Houghton; Malcolm A. Smith

doi:10.1002/pbc.25329

Initial testing (stage 1) of BAL101553, a novel tubulin binding agent, by the pediatric preclinical testing program

E. Anders Kolb, Richard Gorlick, Stephen T. Keir, John M. Maris, Min H. Kang, C. Patrick Reynolds, Richard B. Lock, Hernan Carol, Jianrong Wu, Raushan T. Kurmasheva, Peter J. Houghton, Malcolm A. Smith

Internal Medicine

Research output: Contribution to journal › Article › peer-review

8 Scopus citations

Abstract

BAL101553 is a highly water soluble prodrug of BAL27862 that arrests tumor cell proliferation and induces cell death in cancer cells through disruption of the microtubule network. In vitro BAL27862 demonstrated potent activity, with the median relative IC₅₀ (rIC₅₀) of 13.8nM (range 5.4-25.2nM). The in vitro activity of BAL27862 against the PPTP cell lines is distinctive from that previously described for vincristine. BAL101553 induced significant differences in EFS distribution compared to control in 16 of 30 (53%) solid tumor xenografts and in two of four (67%) of the evaluable ALL xenografts. No objective responses were observed.

Original language	English
Pages (from-to)	1106-1109
Number of pages	4
Journal	Pediatric Blood and Cancer
Volume	62
Issue number	6
DOIs	https://doi.org/10.1002/pbc.25329
State	Published - Jun 1 2015

Bibliographical note

Publisher Copyright:
© 2014 Wiley Periodicals, Inc.

Funding

Funders	Funder number
National Childhood Cancer Registry – National Cancer Institute	CA108786, NO1-CM-42216
National Childhood Cancer Registry – National Cancer Institute	P30CA021765

Keywords

Developmental therapeutics
Microtubule-binding agents
Preclinical testing
Vascular-disrupting agents

ASJC Scopus subject areas

Pediatrics, Perinatology, and Child Health
Hematology
Oncology

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1002/pbc.25329

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Kolb, E. A., Gorlick, R., Keir, S. T., Maris, J. M., Kang, M. H., Reynolds, C. P., Lock, R. B., Carol, H., Wu, J., Kurmasheva, R. T., Houghton, P. J., & Smith, M. A. (2015). Initial testing (stage 1) of BAL101553, a novel tubulin binding agent, by the pediatric preclinical testing program. Pediatric Blood and Cancer, 62(6), 1106-1109. https://doi.org/10.1002/pbc.25329

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abstract = "BAL101553 is a highly water soluble prodrug of BAL27862 that arrests tumor cell proliferation and induces cell death in cancer cells through disruption of the microtubule network. In vitro BAL27862 demonstrated potent activity, with the median relative IC50 (rIC50) of 13.8nM (range 5.4-25.2nM). The in vitro activity of BAL27862 against the PPTP cell lines is distinctive from that previously described for vincristine. BAL101553 induced significant differences in EFS distribution compared to control in 16 of 30 (53%) solid tumor xenografts and in two of four (67%) of the evaluable ALL xenografts. No objective responses were observed.",

keywords = "Developmental therapeutics, Microtubule-binding agents, Preclinical testing, Vascular-disrupting agents",

author = "Kolb, {E. Anders} and Richard Gorlick and Keir, {Stephen T.} and Maris, {John M.} and Kang, {Min H.} and Reynolds, {C. Patrick} and Lock, {Richard B.} and Hernan Carol and Jianrong Wu and Kurmasheva, {Raushan T.} and Houghton, {Peter J.} and Smith, {Malcolm A.}",

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doi = "10.1002/pbc.25329",

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AU - Kolb, E. Anders

AU - Gorlick, Richard

AU - Keir, Stephen T.

AU - Maris, John M.

AU - Kang, Min H.

AU - Reynolds, C. Patrick

AU - Lock, Richard B.

AU - Carol, Hernan

AU - Wu, Jianrong

AU - Kurmasheva, Raushan T.

AU - Houghton, Peter J.

AU - Smith, Malcolm A.

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AB - BAL101553 is a highly water soluble prodrug of BAL27862 that arrests tumor cell proliferation and induces cell death in cancer cells through disruption of the microtubule network. In vitro BAL27862 demonstrated potent activity, with the median relative IC50 (rIC50) of 13.8nM (range 5.4-25.2nM). The in vitro activity of BAL27862 against the PPTP cell lines is distinctive from that previously described for vincristine. BAL101553 induced significant differences in EFS distribution compared to control in 16 of 30 (53%) solid tumor xenografts and in two of four (67%) of the evaluable ALL xenografts. No objective responses were observed.

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KW - Microtubule-binding agents

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KW - Vascular-disrupting agents

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Initial testing (stage 1) of BAL101553, a novel tubulin binding agent, by the pediatric preclinical testing program

Abstract

Bibliographical note

Funding

Keywords

ASJC Scopus subject areas

UN SDGs

Access to Document

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