ACP-5862 is a major active, circulating, pyrrolidine ring-opened metabolite of Acalabrutinib with an IC50 of 5.0 nM for Bruton tyrosine kinase (BTK). ACP‐5862 is a weak time‐dependent inactivator of CYP3A4 and CYP2C8. Acalabrutinib is an orally active, irreversible, and highly selective BTK inhibitor, with an IC50 of 3 nM and EC50 of 8 nM.
| Molecular Weight | 481.51 |
| CAS Number | 2230757-47-6 |
| Solubility (25°C) | DMSO 150 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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.
| Related Products |
|---|
| Izeltabart
Izeltabart is a high-affinity humanized antibody targeting ADAM9. Izeltabart can be used as ADC Antibody for site-specific conjugation with Maytansinoid-based DM21-C to synthesize IMGC936, an Antibody-drug Conjugate with strong anti-cancer activity. IMGC936 exhibits cytotoxicity against ADAM9-positive human tumor cell lines and potent antitumor activity in xenograft tumor models. |
| Cofetuzumab
Cofetuzumab (PF-06523435) is a humanized IgG1-κ monoclonal antibody targeting PTK7. |
| Crizanlizumab
Crizanlizumab is an anti-P-selectin monoclonal antibody. Crizanlizumab binds to P-selectin and blocks its interaction with P-selectin glycoprotein ligand 1 (PSGL-1). Crizanlizumab prevents vaso-occlusive crises (VOCs). |
| M3554 (anti-GD2 ADC)
M3554 is a novel anti-GD2 ADC designed based on humanized ch14.18 anti-GD2 antibody. M3554 has anti-tumor activity. |
| OGT2115
OGT2115 is a potent, cell-permeable and orally active heparanase inhibitor with an IC50 of 0.4 μM. OGT2115 has anti-angiogenic properties (IC50 = 1 μM). |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
