1. Protein Tyrosine Kinase/RTK
  2. Btk
    Itk

SNS-062 

Cat. No.: HY-101941 Purity: 98.88%
Handling Instructions

SNS-062 is a potent, noncovalent BTK and ITK inhibitor, with Kd of 0.3 nM and 2.2 nM, respectively; with IC50 of 24 nM for ITK.

For research use only. We do not sell to patients.
SNS-062 Chemical Structure

SNS-062 Chemical Structure

CAS No. : 1270014-40-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 145 In-stock
5 mg USD 132 In-stock
10 mg USD 192 In-stock
50 mg USD 576 In-stock
100 mg USD 936 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

SNS-062 is a potent, noncovalent BTK and ITK inhibitor, with Kd of 0.3 nM and 2.2 nM, respectively; with IC50 of 24 nM for ITK.

IC50 & Target

IC50: 24 nM (ITK)[2]
Kd: 0.3 nM (BTK), 2.2 nM (ITK)[1]

In Vitro

SNS-062 inhibits pBTK in human whole blood with an average IC50 of 50 nM. SNS-062 inhibits WT and C481S BTK with similar IC50s (pBTK IC50s: WT BTK 2.9 nM, C481S BTK 4.4 nM)[1]. In a recombinant kinase assay, IC50s of SNS-062 against WT BTK and C481S BTK are 4.6 nM and 1.1 nM. SNS-062 retains activity against the mutated BTK variant. SNS-062 is six times more potent than ibrutinib and greater than 640 times more potent than acalabrutinib against C481S BTK. SNS-062 demonstrates dose-dependent inhibition of BTK in primary patient CLL cells comparable to ibrutinib via immunoblot for BTK phosphorylation. SNS-062 decreases viability of primary CLL cells in the presence of HS5 stromal protection by 5.5%[2].

In Vivo

SNS-062 has good oral bioavailability in rat and dog (%F ≥ 40%) and a terminal half-life of 5 to 6 hours. SNS-062 is well tolerated with continuous drug levels and at exposures much greater than those achieved for ibrutinib[1].

Clinical Trial
References
Molecular Weight

384.86

Formula

C₁₉H₂₁ClN₆O

CAS No.

1270014-40-8

SMILES

O=C(NC1CN(C2=C3C(NC=C3)=NC=N2)CCC1)CNC4=CC=CC(Cl)=C4

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

Solvent & Solubility

DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
SNS-062
Cat. No.:
HY-101941
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