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MedKoo Cat#: 598573 | Name: Leniolisib phosphate
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Leniolisib, also known CDZ173, is a potent and selective phosphoinositide 3-kinase inhibitor (PI3Kδ inhibitor), which means it blocks a form of the protein called phosphoinositide 3-kinase delta (PI3Kδ) that is overactive in activated PI3K delta syndrome. By inhibiting PI3Kδ, leniolisib helps normalize immune function as measured by a significant increase in number of immune response generating B cells and reduction in size of lymph nodes.

Chemical Structure

Leniolisib phosphate
Leniolisib phosphate
CAS#1354691-97-6 (phosphate)

Theoretical Analysis

MedKoo Cat#: 598573

Name: Leniolisib phosphate

CAS#: 1354691-97-6 (phosphate)

Chemical Formula: C21H28F3N6O6P

Exact Mass: 0.0000

Molecular Weight: 548.46

Elemental Analysis: C, 45.99; H, 5.15; F, 10.39; N, 15.32; O, 17.50; P, 5.65

Price and Availability

Size Price Availability Quantity
100mg USD 1,250.00 2 months
200mg USD 1,950.00 2 months
500mg USD 3,650.00 2 months
1g USD 4,950.00 2 months
2g USD 7,950.00 2 months
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Related CAS #
1354690-24-6 (free base) 1354691-97-6 (phosphate)
Synonym
Leniolisib phosphate; Leniolisib monophosphate; CDZ-173; CDZ 173; CDZ173;
IUPAC/Chemical Name
(S)-1-(3-((6-(6-methoxy-5-(trifluoromethyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yl)amino)pyrrolidin-1-yl)propan-1-one phosphate
InChi Key
XXEDEGOAYSGNPS-ZOWNYOTGSA-N
InChi Code
InChI=1S/C21H25F3N6O2.H3O4P/c1-3-18(31)30-6-4-13(10-30)28-19-15-11-29(7-5-17(15)26-12-27-19)14-8-16(21(22,23)24)20(32-2)25-9-14;1-5(2,3)4/h8-9,12-13H,3-7,10-11H2,1-2H3,(H,26,27,28);(H3,1,2,3,4)/t13-;/m0./s1
SMILES Code
CCC(N1C[C@@H](NC2=C(CN(C3=CC(C(F)(F)F)=C(OC)N=C3)CC4)C4=NC=N2)CC1)=O.O=P(O)(O)O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.03.00
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 548.46 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Pearson D, Garnier M, Luneau A, James AD, Walles M. (19)F-NMR-based determination of the absorption, metabolism and excretion of the oral phosphatidylinositol-3-kinase (PI3K) delta inhibitor leniolisib (CDZ173) in healthy volunteers. Xenobiotica. 2018 Nov 29:1-8. doi: 10.1080/00498254.2018.1523488. [Epub ahead of print] PubMed PMID: 30215545. 2: De Buck S, Kucher K, Hara H, Gray C, Woessner R. CYP3A but not P-gp plays a relevant role in the in vivo intestinal and hepatic clearance of the delta-specific phosphoinositide-3 kinase inhibitor leniolisib. Biopharm Drug Dispos. 2018 Sep;39(8):394-402. doi: 10.1002/bdd.2157. PubMed PMID: 30171694. 3: Chinen J, Cowan MJ. Advances and highlights in primary immunodeficiencies in 2017. J Allergy Clin Immunol. 2018 Oct;142(4):1041-1051. doi: 10.1016/j.jaci.2018.08.016. Epub 2018 Aug 29. PubMed PMID: 30170128; PubMed Central PMCID: PMC6175644. 4: Avery DT, Kane A, Nguyen T, Lau A, Nguyen A, Lenthall H, Payne K, Shi W, Brigden H, French E, Bier J, Hermes JR, Zahra D, Sewell WA, Butt D, Elliott M, Boztug K, Meyts I, Choo S, Hsu P, Wong M, Berglund LJ, Gray P, O'Sullivan M, Cole T, Holland SM, Ma CS, Burkhart C, Corcoran LM, Phan TG, Brink R, Uzel G, Deenick EK, Tangye SG. Germline-activating mutations in PIK3CD compromise B cell development and function. J Exp Med. 2018 Aug 6;215(8):2073-2095. doi: 10.1084/jem.20180010. Epub 2018 Jul 17. PubMed PMID: 30018075; PubMed Central PMCID: PMC6080914. 5: Lozac'h F, Fahrni S, Maria D, Welte C, Bourquin J, Synal HA, Pearson D, Walles M, Camenisch G. Evaluation of cAMS for (14)C microtracer ADME studies: opportunities to change the current drug development paradigm. Bioanalysis. 2018 Mar 1;10(5):321-339. doi: 10.4155/bio-2017-0216. Epub 2018 Feb 16. PubMed PMID: 29451392. 6: Rao VK, Webster S, Dalm VASH, Šedivá A, van Hagen PM, Holland S, Rosenzweig SD, Christ AD, Sloth B, Cabanski M, Joshi AD, de Buck S, Doucet J, Guerini D, Kalis C, Pylvaenaeinen I, Soldermann N, Kashyap A, Uzel G, Lenardo MJ, Patel DD, Lucas CL, Burkhart C. Effective "activated PI3Kδ syndrome"-targeted therapy with the PI3Kδ inhibitor leniolisib. Blood. 2017 Nov 23;130(21):2307-2316. doi: 10.1182/blood-2017-08-801191. Epub 2017 Sep 29. PubMed PMID: 28972011; PubMed Central PMCID: PMC5701526. 7: Hoegenauer K, Soldermann N, Zécri F, Strang RS, Graveleau N, Wolf RM, Cooke NG, Smith AB, Hollingworth GJ, Blanz J, Gutmann S, Rummel G, Littlewood-Evans A, Burkhart C. 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. doi: 10.1021/acsmedchemlett.7b00293. eCollection 2017 Sep 14. PubMed PMID: 28947947; PubMed Central PMCID: PMC5601375.