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> Duvelisib [1201438-56-3]

Duvelisib [1201438-56-3]

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Referentie 10-4788-5mg

Formaat : 5mg

Merk : Focus Biomolecules

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Duvelisib | PI3Kdelta/gamma inhibitor

CAS:
1201438-56-3
Catalog Number:
10-4788
Activity:
PI3Kδ/γ inhibitor/Cancer immunotherapy enhancer
Chemical Name:
8-Chloro-2-phenyl-3-[(1S)-1-(7H-purin-6-ylamino)ethyl]isoquinolin-1-one
Alternative Name:
IPI-145
Molecular Weight:
416.87
Molecular Formula:
C22H17ClN6O
Solubility:
Soluble in DMSO (up to at least 25 mg/ml)
Physical Properties:
White solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Available Options

Size: Quantity 
5 mg$65.00
25 mg$200.00
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Duvelisib (1201438-56-3) is a potent and selective (IC50’s: PI3Kα = 1602nM, PI3Kβ = 85nM, PI3Kδ= 2.5nM, PI3Kγ = 27nM) dual PI3Kδ/γ inhibitor.1 It inhibits B and T cell proliferation, blocks neutrophil migration, and inhibits basophil activation. Duvelisib antagonizes B-cell receptor cross-linking activated pro-survival signals in primary chronic lymphocytic leukemia cells.2 Duvelisib also shows preclinical/clinical activity against other hematologic malignancies such as Non-Hodgkins lymphoma, T-cell lymphoma, and others.3,4 Useful clinical agent for the treatment of various blood cancers. Low-dose treatment of T-cell-inflamed tumor models of head and neck cancers with Duvelisib enhanced responses to PD-L1 blockade via suppression of myeloid-derived suppressor cells.5 Higher doses reversed the effect due to suppression of tumor-infiltrating T lymphocytes

References/Citations:

1) Winkler et al. (2013), PI3K-δ and PI3K-γ Inhibition by IPI-145 Abrogates Immune Response and Suppresses Activity in Autoimmune and Inflammatory Disease Models; Chem. Biol. 20 1309
2) Dong et al. (2014), IPI-145 antagonizes intrinsic and extrinsic survival signals in chronic lymphocytic leukemia cells; Blood 124 3583
3) Flinn et al. (2018), Duvelisib, a novel dual inhibitor of PI3K-δ/γ, is clinically active in advances hematologic malignancies; Blood 131 877
4) Faia et al. (2018), The phosphoinositide-3 kinase (PI3K)-δ,γ inhibitor, duvelisib, shows preclinical synergy with multiple targeted therapies in hematologic malignancies; PLoS One 13 e0200725
5) Davis et al. (2017), Anti-PD-L1 Efficacy Can Be Enhanced by Inhibition of Myeloid-Derived Suppressor Cells with a Selective Inhibitor of PI3Kδ/γ; Cancer Res. 77 2607

CAS:
1201438-56-3
Catalog Number:
10-4788
Activity:
PI3Kδ/γ inhibitor/Cancer immunotherapy enhancer
Chemical Name:
8-Chloro-2-phenyl-3-[(1S)-1-(7H-purin-6-ylamino)ethyl]isoquinolin-1-one
Alternative Name:
IPI-145
Molecular Weight:
416.87
Molecular Formula:
C22H17ClN6O
Solubility:
Soluble in DMSO (up to at least 25 mg/ml)
Physical Properties:
White solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Download 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 restocking/refund fee

Duvelisib (1201438-56-3) is a potent and selective (IC50’s: PI3Kα = 1602nM, PI3Kβ = 85nM, PI3Kδ= 2.5nM, PI3Kγ = 27nM) dual PI3Kδ/γ inhibitor.1 It inhibits B and T cell proliferation, blocks neutrophil migration, and inhibits basophil activation. Duvelisib antagonizes B-cell receptor cross-linking activated pro-survival signals in primary chronic lymphocytic leukemia cells.2 Duvelisib also shows preclinical/clinical activity against other hematologic malignancies such as Non-Hodgkins lymphoma, T-cell lymphoma, and others.3,4 Useful clinical agent for the treatment of various blood cancers. Low-dose treatment of T-cell-inflamed tumor models of head and neck cancers with Duvelisib enhanced responses to PD-L1 blockade via suppression of myeloid-derived suppressor cells.5 Higher doses reversed the effect due to suppression of tumor-infiltrating T lymphocytes

References/Citations:

1) Winkler et al. (2013), PI3K-δ and PI3K-γ Inhibition by IPI-145 Abrogates Immune Response and Suppresses Activity in Autoimmune and Inflammatory Disease Models; Chem. Biol. 20 1309
2) Dong et al. (2014), IPI-145 antagonizes intrinsic and extrinsic survival signals in chronic lymphocytic leukemia cells; Blood 124 3583
3) Flinn et al. (2018), Duvelisib, a novel dual inhibitor of PI3K-δ/γ, is clinically active in advances hematologic malignancies; Blood 131 877
4) Faia et al. (2018), The phosphoinositide-3 kinase (PI3K)-δ,γ inhibitor, duvelisib, shows preclinical synergy with multiple targeted therapies in hematologic malignancies; PLoS One 13 e0200725
5) Davis et al. (2017), Anti-PD-L1 Efficacy Can Be Enhanced by Inhibition of Myeloid-Derived Suppressor Cells with a Selective Inhibitor of PI3Kδ/γ; Cancer Res. 77 2607