1. Protein Tyrosine Kinase/RTK
  2. Btk

PRN1008 

Cat. No.: HY-112166 Purity: 99.49%
Handling Instructions

PRN1008 is a reversible covalent inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC50 of 1.3 nM.

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

PRN1008 Chemical Structure

PRN1008 Chemical Structure

CAS No. : 1575596-29-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 513 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1500 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2100 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

PRN1008 is a reversible covalent inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC50 of 1.3 nM.

IC50 & Target[1][2]

BTK

1.3 nM (IC50)

BMX

1.0 nM (IC50)

ITK

440 nM (IC50)

TEC

0.8 nM (IC50)

RLK

1.2 nM (IC50)

BLK

6.3 nM (IC50)

EGFR

520 nM (IC50)

ERBB2

3900 nM (IC50)

ERBB4

11.3 nM (IC50)

In Vitro

PRN1008 is a reversible covalent inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC50 of 1.3±0.5 nM. PRN1008 is also found to be highly selectively when tested in a panel of 251 other kinases. Cysteine targeting of BTK by PRN1008 results in a slow off-rate demonstrated by retention of 79±2% of binding to BTK in PBMC 18 hours after washing away the compound in vitro. The covalent cysteine binding is completely reversible after denaturation of the target. Anti-IgM induces human B cell proliferation (10% serum) and B cell CD69 expression are inhibited by PRN1008 with IC50 of 5±2.4 nM and 123±38 nM, respectively[2].

In Vivo

In vivo PRN1008 demonstrates enduring pharmacodynamic effects after the compound has cleared from circulation, consistent with extended target residence time. PRN1008 also reverses and completely suppresses collagen-induced arthritis in rats in a dose dependent manner which allows correlation of target occupancy and disease modification[2].

Clinical Trial
Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5020 mL 7.5102 mL 15.0204 mL
5 mM 0.3004 mL 1.5020 mL 3.0041 mL
10 mM 0.1502 mL 0.7510 mL 1.5020 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

665.76

Formula

C₃₆H₄₀FN₉O₃

CAS No.

1575596-29-0

SMILES

NC1=C2C(C3=C(C=C(OC4=CC=CC=C4)C=C3)F)=NN([[email protected]]5CN(CCC5)C(/C(C#N)=C/C(C)(N6CCN(C7COC7)CC6)C)=O)C2=NC=N1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
PRN1008
Cat. No.:
HY-112166
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PRN1008

Cat. No.: HY-112166