Tenalisib
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MedKoo CAT#: 206093

CAS#: 1639417-53-0

Description: 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

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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 Quantity
10.0mg USD 190.0 2 Weeks
25.0mg USD 450.0 2 Weeks
50.0mg USD 750.0 2 Weeks
100.0mg USD 1350.0 2 Weeks
200.0mg USD 1950.0 2 Weeks
500.0mg USD 3250.0 2 Weeks
1.0g USD 4450.0 2 Weeks
2.0g USD 7450.0 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

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.

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

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1. Swaroop Vakkalanka, Srikant Viswanadha, Eugenio Gaudio, Emanuele Zucca, Francesco Bertoni, Elena Bernasconi, Davide Rossi, Anastasios Stathis, Dual PI3Kδ/γ Inhibition By RP6530 Induces Apoptosis and Cytotoxicity In B-Lymphoma Cells. Blood October 21, 2013 vol. 122 no. 21 4411.



Additional Information

  
 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).