Tenalisib | RP-6530 | 1639417-53-0 | 1693773-94-2 | PI3Kδ/γ inhibitor

MedKoo Cat#: 206093 | Name: Tenalisib

Description:

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

Tenalisib, also known as RP6530, is a potent and selective dual PI3Kδ/γ inhibitor that inhibited growth of B-cell lymphoma cell lines with a concomitant reduction in the downstream biomarker, pAKT. Additionally, the compound showed cytotoxicity in a panel of lymphoma primary cells. Findings provide a rationale for future clinical trials in B-cell malignancies.

Chemical Structure

Tenalisib

CAS#1639417-53-0

Theoretical Analysis

MedKoo Cat#: 206093

Name: Tenalisib

CAS#: 1639417-53-0

Chemical Formula: C23H18FN5O2

Exact Mass: 415.1445

Molecular Weight: 415.43

Elemental Analysis: C, 66.50; H, 4.37; F, 4.57; N, 16.86; O, 7.70

Price and Availability

Size	Price	Availability
10mg	USD 150.00	2 Weeks
25mg	USD 250.00	2 Weeks
50mg	USD 450.00	2 Weeks
100mg	USD 750.00	2 Weeks
200mg	USD 1,350.00	2 Weeks
500mg	USD 2,950.00	2 Weeks
1g	USD 4,450.00	2 Weeks
2g	USD 7,450.00	2 Weeks

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Related CAS #

1639417-53-0 1693773-94-2

Synonym

RP6530; RP-6530; RP 6530; Tenalisib.

IUPAC/Chemical Name

(S)-2-(1-((7H-purin-6-yl)amino)propyl)-3-(3-fluorophenyl)-4H-chromen-4-one

InChi Key

HDXDQPRPFRKGKZ-INIZCTEOSA-N

InChi Code

InChI=1S/C23H18FN5O2/c1-2-16(29-23-19-22(26-11-25-19)27-12-28-23)21-18(13-6-5-7-14(24)10-13)20(30)15-8-3-4-9-17(15)31-21/h3-12,16H,2H2,1H3,(H2,25,26,27,28,29)/t16-/m0/s1

SMILES Code

O=C1C(C2=CC=CC(F)=C2)=C([C@@H](NC3=C4NC=NC4=NC=N3)CC)OC5=C1C=CC=C5

Appearance

white 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, not in water

Shelf Life

>2 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

2934.99.9001

More Info

RP6530 demonstrated high potency against PI3Kδ (IC50 =24.5 nM) and γ (IC50 = 33.2 nM) enzymes with selectivity over α (>300-fold) and β (>100-fold) isoforms. Cellular potency was confirmed in target-specific assays, namely anti-FcεR1-(EC50=37.8 nM) or fMLP (EC50 = 39.0 nM) induced CD63 expression in human whole blood basophils, LPS induced CD19+ cell proliferation in human whole blood (EC50=250 nM), and LPS induced CD45R+ cell proliferation in mouse whole blood (EC50=101 nM).

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 415.43 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.

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: Iyer SP, Huen A, Ai WZ, Jagadeesh D, Lechowicz MJ, Okada C, Feldman TA, Ghione P, Alderuccio JP, Champion R, Kim SH, Mohrbacher A, Routhu KV, Barde P, Nair AM, Haverkos BM. Safety and efficacy of tenalisib in combination with romidepsin in patients with relapsed/refractory T-cell lymphoma: results from a phase I/II open-label multicenter study. Haematologica. 2024 Jan 1;109(1):209-219. doi: 10.3324/haematol.2022.281875. PMID: 37439343; PMCID: PMC10772524. 2: Nguyen CN, Iyer SP, Duvic M, Barde PJ, Nair A, Routhu KV, Huen AO. Complete Response to tenalisib and romidepsin with long-term maintenance using tenalisib monotherapy in a patient with relapsed and refractory sézary syndrome. Invest New Drugs. 2023 Apr;41(2):350-355. doi: 10.1007/s10637-022-01315-6. Epub 2023 Apr 1. PMID: 37004644. 3: Huen A, Haverkos BM, Zain J, Radhakrishnan R, Lechowicz MJ, Devata S, Korman NJ, Pinter-Brown L, Oki Y, Barde PJ, Nair A, Routhu KV, Viswanadha S, Vakkalanka S, Iyer SP. Phase I/Ib Study of Tenalisib (RP6530), a Dual PI3K δ/γ Inhibitor in Patients with Relapsed/Refractory T-Cell Lymphoma. Cancers (Basel). 2020 Aug 15;12(8):2293. doi: 10.3390/cancers12082293. PMID: 32824175; PMCID: PMC7463651. 4: Carlo-Stella C, Delarue R, Scarfo L, Barde PJ, Nair A, Locatelli SL, Morello L, Magagnoli M, Vakkalanka S, Viswanadha S, Ferreri AJM. A First-in-human Study of Tenalisib (RP6530), a Dual PI3K δ/γ Inhibitor, in Patients With Relapsed/Refractory Hematologic Malignancies: Results From the European Study. Clin Lymphoma Myeloma Leuk. 2020 Feb;20(2):78-86. doi: 10.1016/j.clml.2019.10.013. Epub 2019 Oct 23. PMID: 31761713. 5: Ito Y, Makita S, Tobinai K. Development of new agents for peripheral T-cell lymphoma. Expert Opin Biol Ther. 2019 Mar;19(3):197-209. doi: 10.1080/14712598.2019.1572746. Epub 2019 Jan 29. PMID: 30658046. 6: Locatelli SL, Careddu G, Serio S, Consonni FM, Maeda A, Viswanadha S, Vakkalanka S, Castagna L, Santoro A, Allavena P, Sica A, Carlo-Stella C. Targeting Cancer Cells and Tumor Microenvironment in Preclinical and Clinical Models of Hodgkin Lymphoma Using the Dual PI3Kδ/γ Inhibitor RP6530. Clin Cancer Res. 2019 Feb 1;25(3):1098-1112. doi: 10.1158/1078-0432.CCR-18-1133. Epub 2018 Oct 23. PMID: 30352904.