Galunisertib | Potent TGFB receptor 1 inhibitor / Cancer immunotherapeutic
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $45.00 | ||
| 25 mg | $140.00 |
Galunisertib (700874-72-2) is a TGF-β kinase (ALK5) antagonist.1 It stimulated hematopoiesis from primary myelodysplastic syndrome bone marrow specimens via downregulation of SMAD2 phosphorylation.2 It has been in clinical trials for treatment of various cancers.3-5 Galunisertib has more recently been used to enhance the anti-neuroblastoma activity of anti-GD2 antibody Dinutuximab with natural killer cells6 and preserved the function of in vitro expanded natural killer cells in AML and colon cancer models7. Galunisertib reversed TGF-β and regulatory T cell mediated suppression of human T cell proliferation. In combination with PD-L1 blockade, it resulted in improved tumor growth inhibition and complete regressions in colon carcinoma models.8
References/Citations:
1) Bueno et al. (2008), Semi-mechanistic modelling of the tumour growth inhibitory effects of LY2157299, a new type I receptor TGF-β kinase antagonist, in mice; Eur. J. Cancer 44 142
2) Zhou et al. (2011), Reduced SMAD7 leads to overactivation of TGF-beta signaling in MDS that can be reversed by a specific inhibitor of TGF-beta receptor I kinase; Cancer Res. 71 955
3) Rodon et al. (2015), First-in-human dose study of the novel transforming growth factor-b-receptor I kinase inhibitor LY2157299 monohydrate in patients with advances cancer and glioma; Clin. Cancer Res. 21 553
4) Herbertz et al. (2015), Clinical development of galunisertib (LY2157299 monohydrate), a small molecule inhibitor of transforming growth factor-beta signaling pathway; Drug Des. Devel. Ther. 9 4479
5) Brandes et al. (2016), A Phase II randomized study of galunisertib monotherapy or galunisertib plus lomustine compared with lomustine monotherapy in patients with recurrent glioblastoma; Neuro. Oncol. 18 1146
6) Tran et al. (2017), TGFβR1 Blockade with Galunisertib (LY2157299 Enhances Anti-Neuroblastoma Activity of the Anti-GD2 Antibody Dinutuximab (ch14.18) with Natural Killer Cells; Clin. Cancer Res. 23 804
7) Otegbeye et al. (2018), Inhibiting TGF-beta signaling preserves the function of highly activated, in vitro expanded natural killer cells in AML and colon cancer models; PLoS One 13 e0197008
8) Holmgaard et al. (2018), Targeting the TGFβ pathway with galunisertib, a TGFβRI small molecule inhibitor, promotes anti-tumor immunity leading to durable, complete response, as monotherapy and in combination with checkpoint blockade; J. Immunother. Cancer 6 47
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
Galunisertib (700874-72-2) is a TGF-β kinase (ALK5) antagonist.1 It stimulated hematopoiesis from primary myelodysplastic syndrome bone marrow specimens via downregulation of SMAD2 phosphorylation.2 It has been in clinical trials for treatment of various cancers.3-5 Galunisertib has more recently been used to enhance the anti-neuroblastoma activity of anti-GD2 antibody Dinutuximab with natural killer cells6 and preserved the function of in vitro expanded natural killer cells in AML and colon cancer models7. Galunisertib reversed TGF-β and regulatory T cell mediated suppression of human T cell proliferation. In combination with PD-L1 blockade, it resulted in improved tumor growth inhibition and complete regressions in colon carcinoma models.8
References/Citations:
1) Bueno et al. (2008), Semi-mechanistic modelling of the tumour growth inhibitory effects of LY2157299, a new type I receptor TGF-β kinase antagonist, in mice; Eur. J. Cancer 44 142
2) Zhou et al. (2011), Reduced SMAD7 leads to overactivation of TGF-beta signaling in MDS that can be reversed by a specific inhibitor of TGF-beta receptor I kinase; Cancer Res. 71 955
3) Rodon et al. (2015), First-in-human dose study of the novel transforming growth factor-b-receptor I kinase inhibitor LY2157299 monohydrate in patients with advances cancer and glioma; Clin. Cancer Res. 21 553
4) Herbertz et al. (2015), Clinical development of galunisertib (LY2157299 monohydrate), a small molecule inhibitor of transforming growth factor-beta signaling pathway; Drug Des. Devel. Ther. 9 4479
5) Brandes et al. (2016), A Phase II randomized study of galunisertib monotherapy or galunisertib plus lomustine compared with lomustine monotherapy in patients with recurrent glioblastoma; Neuro. Oncol. 18 1146
6) Tran et al. (2017), TGFβR1 Blockade with Galunisertib (LY2157299 Enhances Anti-Neuroblastoma Activity of the Anti-GD2 Antibody Dinutuximab (ch14.18) with Natural Killer Cells; Clin. Cancer Res. 23 804
7) Otegbeye et al. (2018), Inhibiting TGF-beta signaling preserves the function of highly activated, in vitro expanded natural killer cells in AML and colon cancer models; PLoS One 13 e0197008
8) Holmgaard et al. (2018), Targeting the TGFβ pathway with galunisertib, a TGFβRI small molecule inhibitor, promotes anti-tumor immunity leading to durable, complete response, as monotherapy and in combination with checkpoint blockade; J. Immunother. Cancer 6 47
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1-855-FOCUS21
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