1. Protein Tyrosine Kinase/RTK
    Immunology/Inflammation
  2. Btk
    BMX Kinase
    Toll-like Receptor (TLR)
  3. Poseltinib

Poseltinib (Synonyms: HM71224; LY3337641)

Cat. No.: HY-109010 Purity: 98.01%
Handling Instructions

Poseltinib, an orally active, selective and irreversible Bruton’s tyrosine kinase (BTK) inhibitor (IC50 =1.95 nM), with 0.3, 2.3 and 2.4-fold selectivity for BTK over BMX, TEC and TXK, respectively. Poseltinib can covalently bind to the active site (cysteine 481 residue) of BTK, and reveales potent inhibition of B cell receptor (BCR), Fc receptor (FcR), Toll-like receptor (TLR) mediated signaling.

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

Poseltinib Chemical Structure

Poseltinib Chemical Structure

CAS No. : 1353552-97-2

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10 mg USD 320 In-stock
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50 mg USD 800 In-stock
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Description

Poseltinib, an orally active, selective and irreversible Bruton’s tyrosine kinase (BTK) inhibitor (IC50 =1.95 nM), with 0.3, 2.3 and 2.4-fold selectivity for BTK over BMX, TEC and TXK, respectively. Poseltinib can covalently bind to the active site (cysteine 481 residue) of BTK, and reveales potent inhibition of B cell receptor (BCR), Fc receptor (FcR), Toll-like receptor (TLR) mediated signaling[1].

IC50 & Target

IC50: 1.95 nM (BTK)[1]

Clinical Trial
Molecular Weight

470.52

Formula

C₂₆H₂₆N₆O₃

CAS No.

1353552-97-2

SMILES

O=C(C=C)NC1=CC=CC(OC2=C(OC=C3)C3=NC(NC4=CC=C(N5CCN(C)CC5)C=C4)=N2)=C1

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 (212.53 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1253 mL 10.6265 mL 21.2531 mL
5 mM 0.4251 mL 2.1253 mL 4.2506 mL
10 mM 0.2125 mL 1.0627 mL 2.1253 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 7.5 mg/mL (15.94 mM); Clear solution

  • 2.

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

    Solubility: ≥ 7.5 mg/mL (15.94 mM); Clear solution

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

PoseltinibHM71224 LY3337641HM 71224HM-71224LY3337641LY 3337641LY-3337641BtkBMX KinaseToll-like Receptor (TLR)Bruton tyrosine kinaseInhibitorinhibitorinhibit

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Poseltinib
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HY-109010
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