Tenalisib (RP6530)

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

MedKoo CAT#: 206093

CAS#: 1639417-53-0 or 1693773-94-2

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.


Price and Availability

Size
Price

1g
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Size
Price

2g
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Size
Price

5g
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RP6530, purity > 98%, is not in stock, may be available through custom synthesis. Minimum 1 gram order is requested. Current shipping out time is about 2 months after order is received. Delivery time: overnight (USA/Canada); 3-5 days (worldwide). Shipping fee: from $30.00 (USA); from $45.00 (Canada); from $70.00 (international).


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 206093
Name: Tenalisib (RP6530)
CAS#: 1639417-53-0 or 1693773-94-2
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


Synonym: RP6530; RP6530; RP 6530; Tenalisib.

IUPAC/Chemical Name: (S)-2-(1-((7H-purin-6-yl)amino)propyl)-3-(3-fluorophenyl)-4H-chromen-4-one

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


Technical Data

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).

Harmonized System Code:
293490


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).
 
 


References

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.