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  3. PI3Kδ-IN-1

PI3Kδ-IN-1 

Cat. No.: HY-101921 Purity: 99.35%
Handling Instructions

PI3Kδ-IN-1 is a potent, selective, and efficacious PI3Kδ inhibitor with an IC50 of 1.7 nM.

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

PI3Kδ-IN-1 Chemical Structure

PI3Kδ-IN-1 Chemical Structure

CAS No. : 1911564-39-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 311 In-stock
Estimated Time of Arrival: December 31
5 mg USD 300 In-stock
Estimated Time of Arrival: December 31
10 mg USD 480 In-stock
Estimated Time of Arrival: December 31
25 mg USD 950 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1450 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2250 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

PI3Kδ-IN-1 is a potent, selective, and efficacious PI3Kδ inhibitor with an IC50 of 1.7 nM.

IC50 & Target

IC50: 1.7 nM (PI3Kδ)[1]

In Vitro

PI3Kδ-IN-1 (compound 52) shows >100-fold selectivity over the other PI3K isoforms. Kinome selectivity is also excellent with >660-fold selectivity over MNK1 and others in HTRF assays. Importantly, PI3Kδ-IN-1 has an improved human/rodent in vitro stability correlation and a good permeability profile[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PI3Kδ-IN-1 (2, 5 mg/kg, orally b.i.d. for 42 days) shows greater than 50% suppression of paw swelling in mice. PI3Kδ-IN-1 has an EC50 of 10 nM at 24 h (ED50 of ∼1.25 mg/kg) in mice[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male DBA/1 mice (20−25g)[1]
Dosage: 0.5, 2, 5 mg/kg
Administration: Oral b.i.d. for 42 days,
Result: A dose dependent reduction of the clinical score was observed. Doses of 2 and 5 mg/kg showed greater than 50% suppression of paw swelling[1].
Molecular Weight

471.44

Formula

C₂₂H₂₀F₃N₇O₂

CAS No.
SMILES

NC1=NC=NN2C1=C(C(F)(F)F)C=C2C3=CC=C(C#N)C(N4CCN(C(C)=O)C(C)(C)C4=O)=C3

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 : 62.5 mg/mL (132.57 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1212 mL 10.6058 mL 21.2116 mL
5 mM 0.4242 mL 2.1212 mL 4.2423 mL
10 mM 0.2121 mL 1.0606 mL 2.1212 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: 2.08 mg/mL (4.41 mM); Suspended solution; Need ultrasonic

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (4.41 mM); Clear solution

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

PI3Kδ-IN-1PI3KPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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PI3Kδ-IN-1
Cat. No.:
HY-101921
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