Initial testing (stage 1) of SGI-1776, a PIM1 kinase inhibitor, by the pediatric preclinical testing program

Vandana Batra; John M. Maris; Min H. Kang; C. Patrick Reynolds; Peter J. Houghton; Denise Alexander; E. Anders Kolb; Richard Gorlick; Stephen T. Keir; Hernan Carol; Richard Lock; Catherine A. Billups; Malcolm A. Smith

doi:10.1002/pbc.23364

Initial testing (stage 1) of SGI-1776, a PIM1 kinase inhibitor, by the pediatric preclinical testing program

Vandana Batra
, John M. Maris
, Min H. Kang
, C. Patrick Reynolds
, Peter J. Houghton
, Denise Alexander
, E. Anders Kolb
, Richard Gorlick
, Stephen T. Keir
, Hernan Carol
, Richard Lock
, Catherine A. Billups
, Malcolm A. Smith

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

24 Scopus citations

Abstract

The PIM kinase inhibitor, SGI-1776, was tested against the PPTP in vitro (1.0nM-10μM) and in vivo panels (148mg/kg daily×5 days for 3 weeks). SGI-1776 exhibited cytotoxic activity in vitro with a median relative IC ₅₀ of 3.1μM. SGI-1776 induced significant differences in EFS distribution in vivo in 9 of 31 solid tumor xenografts and in 1 of 8 of the evaluable ALL xenografts. SGI-1776 induced tumor growth inhibition meeting criteria for intermediate EFS T/C activity in 1 of 39 evaluable models. In contrast, SGI-1776 induced complete responses of subcutaneous MV4;11 (B myeloid leukemia). Pediatr Blood Cancer 2012;59:749-752.

Original language	English (US)
Pages (from-to)	749-752
Number of pages	4
Journal	Pediatric Blood and Cancer
Volume	59
Issue number	4
DOIs	https://doi.org/10.1002/pbc.23364
State	Published - Oct 2012
Externally published	Yes

Keywords

Developmental therapeutics
Kinase inhibitors
Preclinical testing

ASJC Scopus subject areas

Hematology
Oncology
Pediatrics, Perinatology, and Child Health

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10.1002/pbc.23364

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Batra, V., Maris, J. M., Kang, M. H., Reynolds, C. P., Houghton, P. J., Alexander, D., Kolb, E. A., Gorlick, R., Keir, S. T., Carol, H., Lock, R., Billups, C. A., & Smith, M. A. (2012). Initial testing (stage 1) of SGI-1776, a PIM1 kinase inhibitor, by the pediatric preclinical testing program. Pediatric Blood and Cancer, 59(4), 749-752. https://doi.org/10.1002/pbc.23364

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title = "Initial testing (stage 1) of SGI-1776, a PIM1 kinase inhibitor, by the pediatric preclinical testing program",

abstract = "The PIM kinase inhibitor, SGI-1776, was tested against the PPTP in vitro (1.0nM-10μM) and in vivo panels (148mg/kg daily×5 days for 3 weeks). SGI-1776 exhibited cytotoxic activity in vitro with a median relative IC 50 of 3.1μM. SGI-1776 induced significant differences in EFS distribution in vivo in 9 of 31 solid tumor xenografts and in 1 of 8 of the evaluable ALL xenografts. SGI-1776 induced tumor growth inhibition meeting criteria for intermediate EFS T/C activity in 1 of 39 evaluable models. In contrast, SGI-1776 induced complete responses of subcutaneous MV4;11 (B myeloid leukemia). Pediatr Blood Cancer 2012;59:749-752.",

keywords = "Developmental therapeutics, Kinase inhibitors, Preclinical testing",

author = "Vandana Batra and Maris, \{John M.\} and Kang, \{Min H.\} and Reynolds, \{C. Patrick\} and Houghton, \{Peter J.\} and Denise Alexander and Kolb, \{E. Anders\} and Richard Gorlick and Keir, \{Stephen T.\} and Hernan Carol and Richard Lock and Billups, \{Catherine A.\} and Smith, \{Malcolm A.\}",

year = "2012",

month = oct,

doi = "10.1002/pbc.23364",

language = "English (US)",

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AU - Batra, Vandana

AU - Maris, John M.

AU - Kang, Min H.

AU - Reynolds, C. Patrick

AU - Houghton, Peter J.

AU - Alexander, Denise

AU - Kolb, E. Anders

AU - Gorlick, Richard

AU - Keir, Stephen T.

AU - Carol, Hernan

AU - Lock, Richard

AU - Billups, Catherine A.

AU - Smith, Malcolm A.

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AB - The PIM kinase inhibitor, SGI-1776, was tested against the PPTP in vitro (1.0nM-10μM) and in vivo panels (148mg/kg daily×5 days for 3 weeks). SGI-1776 exhibited cytotoxic activity in vitro with a median relative IC 50 of 3.1μM. SGI-1776 induced significant differences in EFS distribution in vivo in 9 of 31 solid tumor xenografts and in 1 of 8 of the evaluable ALL xenografts. SGI-1776 induced tumor growth inhibition meeting criteria for intermediate EFS T/C activity in 1 of 39 evaluable models. In contrast, SGI-1776 induced complete responses of subcutaneous MV4;11 (B myeloid leukemia). Pediatr Blood Cancer 2012;59:749-752.

KW - Developmental therapeutics

KW - Kinase inhibitors

KW - Preclinical testing

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AN - SCOPUS:84864928386

SN - 1545-5009

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JF - Pediatric Blood and Cancer

IS - 4

ER -

Initial testing (stage 1) of SGI-1776, a PIM1 kinase inhibitor, by the pediatric preclinical testing program

Abstract

Keywords

ASJC Scopus subject areas

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