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Tenalisib (Synonyms: RP6530)

Cat. No.: HY-17645 Purity: 99.09% ee.: 98.51%
Handling Instructions

Tenalisib (RP6530) is a novel, potent, and selective PI3Kδ and PI3Kγ inhibitor with IC50 values of 25 and 33 nM, respectively.

For research use only. We do not sell to patients.

Tenalisib Chemical Structure

Tenalisib Chemical Structure

CAS No. : 1639417-53-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 174 In-stock
Estimated Time of Arrival: December 31
1 mg USD 90 In-stock
Estimated Time of Arrival: December 31
5 mg USD 190 In-stock
Estimated Time of Arrival: December 31
10 mg USD 290 In-stock
Estimated Time of Arrival: December 31
25 mg USD 590 In-stock
Estimated Time of Arrival: December 31
50 mg USD 890 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1500 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Tenalisib (RP6530) is a novel, potent, and selective PI3Kδ and PI3Kγ inhibitor with IC50 values of 25 and 33 nM, respectively.

IC50 & Target[1]

PI3Kδ

25 nM (IC50)

PI3Kγ

33 nM (IC50)

In Vitro

Tenalisib shows selectivity over PI3K α (>300-fold) and β (>100-fold) isoforms. Tenalisib exhibits modest proliferation inhibition (33-46% inhibition @ 10 μM) in both HEL-RS and HEL-RR cells. Addition of 10 μM tenalisib to ruxolitinib is synergistic resulting in a near-complete inhibition of proliferation (>90% for HEL-RS and >70% for HEL-RR). Addition of 5 μM tenalisib, 4 h prior to the addition of ruxolitinib results in a significant reduction in EC50of ruxolitinib (5.8 μM) in HEL-RR cells. Incubation of 10 μM tenalisib with ruxolitinib for 72 h increases the percent of apoptotic cells (55% in HEL-RS and 37% in HEL-RR) compared to either agent alone (16-27% in HEL-RS and 17-21% in HEL-RR)[1].

In Vivo

Tenalisib has been well tolerated in subjects with heavily pre-treated relapsed/refractory hematologic malignancies. Reported toxicities are manageable with no DLTs. Single agent activity is evident in difficult-to-treat subjects at ≥ 200 mg BID[2].

Clinical Trial
Molecular Weight

415.42

Formula

C₂₃H₁₈FN₅O₂

CAS No.

1639417-53-0

SMILES

O=C1C(C2=CC=CC(F)=C2)=C([[email protected]@H](NC3=C4NC=NC4=NC=N3)CC)OC5=CC=CC=C15

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (240.72 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4072 mL 12.0360 mL 24.0720 mL
5 mM 0.4814 mL 2.4072 mL 4.8144 mL
10 mM 0.2407 mL 1.2036 mL 2.4072 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.09% ee.: 98.51%

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Keywords:

TenalisibRP6530RP 6530RP-6530PI3KPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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Tenalisib
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