Leniolisib phosphate

SKU:BHB21902450
Research Validated
Overview
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Leniolisib phosphate (CAS 1354691-97-6) is an inhibitor supplied as a solid. Reported to act on PI3Kδ, PI3Kα, PI3Kβ. Relevant to PI3K/Akt/mTOR research. Molecular formula C21H28F3N6O6P, molecular weight 548.45 g/mol.
Purity 98.88%
CAS Number 1354691-97-6
Molecular Weight 548.45 g/mol
Form Solid
Target PI3Kδ, PI3Kα, PI3Kβ, PI3Kγ, DNA-PK
Storage -20°C as supplied; in solvent -80°C
Options selector
Catalog no. Size
HY-17635A-5MG 5 mg
HY-17635A-10MG 10 mg
HY-17635A-25MG 25 mg
HY-17635A-50MG 50 mg
HY-17635A-100MG 100 mg
HY-17635A-200MG 200 mg
HY-17635A-500MG 500 mg
HY-17635A-1MLX10MM 1 mL x 10 mM (in DMSO)
Available Options

Select the variant that best fits your experiment. Availability and lead time may vary by option.

  • Options: Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 200 mg, 500 mg, 1 mL x 10 mM (in DMSO)
  • Lead time: varies by selected option.
  • Storage: -20°C, sealed storage, away from moisture. In solvent: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture).
  • Shipping: Room temperature in continental US; may vary elsewhere.
  • Upon receipt: transfer to -20°C as soon as possible.
Field Specification
Target PI3Kδ, PI3Kα, PI3Kβ, PI3Kγ, DNA-PK
Alternative names CDZ173 phosphate
CAS no. 1354691-97-6
Applications
  • Functional Assay (In Vitro)
Molecular weight 548.45
Molecular formula C21H28F3N6O6P
Purity 98.88%
SMILES CCC(N1C[C@H](CC1)NC2=C3CN(CCC3=NC=N2)C4=CC(C(F)(F)F)=C(N=C4)OC)=O.O=P(O)(O)O
Form Solid
Storage -20°C, sealed storage, away from moisture. In solvent: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture).
Shipping Room temperature in continental US; may vary elsewhere.
Catalog no. (Mfr.) HY-17635A
Main SKU BHB21902450
Inhibitors

Compound Overview

Leniolisib phosphate, also known as CDZ173 phosphate, is a potent, selective PI3Kδ inhibitor with potential for the treatment of immunodeficiency disorders. It is supplied as a white to off-white solid (C21H28F3N6O6P, MW 548.45) at 98.88% purity.

Physical & Chemical Properties

CAS Number 1354691-97-6
Molecular Formula C21H28F3N6O6P
Molecular Weight 548.45 g/mol
Purity 98.88%
Appearance Solid
Color White to off-white
SMILES CCC(N1C[C@H](CC1)NC2=C3CN(CCC3=NC=N2)C4=CC(C(F)(F)F)=C(N=C4)OC)=O.O=P(O)(O)O
Target PI3Kδ, PI3Kα, PI3Kβ, PI3Kγ, DNA-PK
Signaling Pathway PI3K/Akt/mTOR
Solubility In Vitro: H2O: 100 mg/mL (182.33 mM; Requires sonication)
DMSO: 100 mg/mL (182.33 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Storage -20°C, sealed storage, away from moisture. In solvent: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture).
Shipping Room temperature in continental US; may vary elsewhere.

Biological Activity

IC50 & Target[1]

PI3Kδ

11 nM (IC50)

PI3Kα

280 nM (IC50)

PI3Kβ

480 nM (IC50)

PI3Kγ

2.57 nM (IC50)

DNA-PK

880 nM (IC50)

Literature Cited

Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.

[1]. Rao V, et al. Effective 'Activated PI3Kd Syndrome' -targeted therapy with PI3Kd inhibitor leniolisib. The New England journal of medicine: NEJM. ISSN 0028-4793; 1533-4406

[2]. Hoegenauer K, et al. Discovery of CDZ173 (Leniolisib), Representing a Structurally Novel Class of PI3K Delta-Selective Inhibitors. ACS Med Chem Lett. 2017 Aug 25;8(9):975-980.

Safety

For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.

In Vitro

SolventSolubilityNotes
H2O100 mg/mL (182.33 mM)requires sonication
DMSO100 mg/mL (182.33 mM)requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility)

Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); sealed storage, away from moisture; avoid repeated freeze-thaw cycles.

If water is used as the stock solvent, dilute to the working solution and sterilize it through a 0.22 μm filter before use.

Data provided by the manufacturer.

In Vitro

In cell lines and patient-derived lymphocytes expressing the APDS mutant p110δ, pathway activity increases, as measured by phosphorylation of AKT or S6, and Leniolisib phosphate suppresses this increase in a concentration-dependent manner[1].

Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.

Q.Why is there no price on some sizes?
A.Availability and lead time for those sizes are confirmed on inquiry. Send us the size you need and we will come back with price and lead time.
Q.Can this be used in humans or for diagnostics?
A.No. This product is supplied For Research Use Only. It is not for diagnostic or therapeutic procedures and not for human or veterinary use.

Need this compound in a format that drops straight into your assay? We can tailor formulation, chemistry, and documentation so your results stay consistent across runs and re-orders.

  • Format options: solid or pre-dissolved solution (choose solvent), target concentration, aliquots, light/moisture-protected packaging
  • Chemistry options: free base/acid vs salt forms, hydrate/solvate preference, stereoisomer control (single enantiomer or racemate), close analogs
  • Add-on labels & handles: D/¹³C/¹⁵N isotopes (LC-MS/internal standards), azide/alkyne or other functional handles for conjugation
  • QC & documentation: standard COA or enhanced analytical pack (HPLC/LC-MS/NMR), chiral purity, residual solvents, water content (KF), method-specific specs
  • Scale & continuity: mg to gram scale, bulk pricing, lot reservation, repeat-order continuity

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Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. Mol Syst Biol 2024 Jan;20(1):28-55. PMID: 38177929

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