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Cat. No.: HY-109029

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Dezapelisib

(Synonyms: INCB040093)

Dezapelisib (NCB040093) is a potent inhibitor of phosphatidylinositol 3-kinase δ (PI3Kδ). Dezapelisib is a promising research strategy for select R/R B-cell lymphomas.

For research use only. We do not sell to patients.

CAS No.: 1262440-25-4
Formula: C₂₀H₁₆FN₇OS
Molecular Weight:421.45

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (271 KB)

Dezapelisib Chemical Structure

CAS No.: 1262440-25-4

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- Clinical Trial
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

Dezapelisib (NCB040093) is a potent inhibitor of phosphatidylinositol 3-kinase δ (PI3Kδ). Dezapelisib is a promising research strategy for select R/R B-cell lymphomas^[1].

All PI3K Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
B-cell	IC₅₀	<0.05 μM Compound: 67	Inhibition of PI3Kdelta in B-cells by proliferation assay Inhibition of PI3Kdelta in B-cells by proliferation assay	[PMID: 22924688]
Pfeiffer	IC₅₀	14 nM Compound: 3; INCB040093	Cytotoxicity against human Pfeiffer cells assessed as reduction in cell viability incubated for 4 days by [3H]-thymidine incorporation based liquid scintillation counter method Cytotoxicity against human Pfeiffer cells assessed as reduction in cell viability incubated for 4 days by [3H]-thymidine incorporation based liquid scintillation counter method	[PMID: 31749910]
Pfeiffer	IC₅₀	66 nM Compound: 3; INCB040093	Cytotoxicity against human Pfeiffer cells assessed as reduction in protein binding adjusted cell viability incubated for 4 days by [3H]-thymidine incorporation based liquid scintillation counter method Cytotoxicity against human Pfeiffer cells assessed as reduction in protein binding adjusted cell viability incubated for 4 days by [3H]-thymidine incorporation based liquid scintillation counter method	[PMID: 31749910]
Sf21	IC₅₀	3751 nM Compound: Dezapelisib	Inhibition of human full length recombinant N-terminal His-tagged PI3Kbeta/p85alpha expressed in baculovirus infected Sf21 insect cells Inhibition of human full length recombinant N-terminal His-tagged PI3Kbeta/p85alpha expressed in baculovirus infected Sf21 insect cells	[PMID: 30530193]
SU-DHL-6	IC₅₀	18 nM Compound: 3; INCB040093	Cytotoxicity against human SUDHL6 cells assessed as reduction in cell viability incubated for 4 days by celltiter glo luminescent assay Cytotoxicity against human SUDHL6 cells assessed as reduction in cell viability incubated for 4 days by celltiter glo luminescent assay	[PMID: 31749910]

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1262440-25-4
Molecular Weight 421.45
Formula C₂₀H₁₆FN₇OS
SMILES

C[C@@H](C1=C(C2=CC(F)=CC=C2)C(N3C(SC=C3C)=N1)=O)NC4=C5C(N=CN5)=NC=N4
Synonyms

INCB040093
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Phillips TJ, et al. Phase 1 study of the PI3Kδ inhibitor INCB040093 ± JAK1 inhibitor itacitinib in relapsed/refractory B-cell lymphoma. Blood. 2018;132(3):293-306. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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