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PCI-29732 is a potent, reversible BTK inhibitor. PCI-29732 blocks B cell antigen receptor (BCR)-mediated gene expression in CD20+ B cells. PCI-29732 inhibits the function of ABCG2 by competitively binding to the ATP-binding site of ABCG2 and enhances the anti-tumor efficacy of substrate chemotherapeutic agents. In vivo, PCI-29732 (20 mg/kg; p.o.; 5 times/3 days) enhances the anticancer efficacy of Topotecan in the H460/MX20 cell xenograft nude mice model.
| 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.
| Molecular Weight | 371.44 |
| Formula | C22H21N5O |
| CAS Number | 330786-25-9 |
| Purity | >99% |
| Solubility | DMSO ≥ 45 mg/mL |
| Storage | at -20°C |
| Related BTK Products |
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| 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. |
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