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Btk inhibitor 2

Cat. No. M8887
Btk inhibitor 2 Structure
Synonym:

BGB-3111

Size Price Availability
5mg USD 100  USD100 4-7 Days
10mg USD 180  USD180 4-7 Days
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

Btk inhibitor 2 (BGB-3111) is a Brutons tyrosine kinase (BTK) inhibitor.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 431.49
Formula C24H25N5O3
CAS Number 1558036-85-3
Purity >98%
Solubility DMSO: 80 mg/mL
Storage at -20°C
References

[1] Ronen Gabizon, et al. A Fast and Clean BTK Inhibitor

[2] Wei Xu, et al. Treatment of relapsed/refractory chronic lymphocytic leukemia/small lymphocytic lymphoma with the BTK inhibitor zanubrutinib: phase 2, single-arm, multicenter study

[3] Qiuyun Luo, et al. A Novel BCL-2 Inhibitor APG-2575 Exerts Synthetic Lethality With BTK or MDM2-p53 Inhibitor in Diffuse Large B-Cell Lymphoma

[4] Constantine S Tam, et al. Phase 1 study of the selective BTK inhibitor zanubrutinib in B-cell malignancies and safety and efficacy evaluation in CLL

[5] Xavier Montalban, et al. Placebo-Controlled Trial of an Oral BTK Inhibitor in Multiple Sclerosis

Related BTK Products
Poseltinib

Poseltinib is an orally active, selective, irreversible small-molecule Bruton tyrosine kinase (BTK) inhibitor with an IC50 of 1.95 nM and 0.3, 2.3, and 2.4 fold selective action against BMX, TEC, and TXK, respectively. Poseltinib covalently binds to the active site of BTK (cysteine 481 residue) and effectively inhibits B cell receptor (BCR), Fc receptor (FcR), and Toll-like receptor (TLR) mediated signaling.

Vecabrutinib

Vecabrutinib (SNS-062) is a potent, non-covalent BTK and ITK inhibitor,Kd The values are 0.3 nM and 2.2 nM, respectively. Vecabrutinib for ITK IC50 The value is 24 nM.

Rilzabrutinib

Rilzabrutinib, also known as PRN1008, is a reversible covalent, selective and oral active inhibitor of Bruton’s Tyrosine Kinase (BTK) with IC50 of 1.3 nM.

Pirtobrutinib (LOXO-305)

Pirtobrutinib (LOXO-305; LY 3527727; RXC-005) is a highly selective and non-covalent next generation BTK inhibitor, which inhibits diverse BTK C481 substitution mutations. Pirtobrutinib is also more than 300-fold selective for BTK versus 370 other kinases.

Remibrutinib (LOU064)

Remibrutinib (LOU064) is a potent and highly selective covalent Inhibitor of Bruton's Tyrosine Kinase (BTK) with IC50 value of 1 nM.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Btk inhibitor 2, BGB-3111 supplier, BTK, inhibitors

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