Rilzabrutinib

SKU: orb1309216

Description

Rilzabrutinib (PRN1008) is a potent, selective, and orally bioavailable reversible covalent inhibitor of Bruton's Tyrosine Kinase (BTK) with an IC50 of 1.3 nM. It is a research tool for investigating BTK's role in immunology and oncology, with applications in both in vitro biochemical assays and in vivo disease models.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1575596-29-0
• MW: 665.76
• Purity: 99.76%
• Formula: C₃₆H₄₀FN₉O₃
• SMILES: CC(C)(\C=C(/C#N)C(=O)N1CCC[C@H](C1)n1nc(-c2ccc(Oc3ccccc3)cc2F)c2c(N)ncnc12)N1CCN(CC1)C1COC1
• Target: HER,EGFR,BTK
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (7.51 mM);DMSO:240 mg/mL (360.49 mM)

Bioactivity

• Target IC50:
  RLK:1.2 nM|ERBB4:11.3 nM|BLK:6.3 nM|ERBB2:3900 nM|FcγR (Monocyte):56 ± 45 nM|BTK:1.3 nM|BCR (B cell):5 ± 2 nM|EGFR:520 nM|TXK:1.2 ± 0.3 nM|ITK:440 nM|TEC:0.8 nM|BMX kinase:1.0 ± 0.1 nM|BTK (Ramos B cell):8 ± 2 nM

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PRN 1008, PRN1008, PRN-1008, RLK, Rilzabrutinib, TEC, HER4, Inhibitor, ERBB4, ERbB2, ERBB2, EGFR, inhibit, ITK, Bruton tyrosine kinase, BLK, BMX, Btk, BTK

Compound Identifiers

PubChem CID

73388818