ITK antagonist (compound 10 n) is a potent, orally active and selective ITK (Interleukin-2 inducible T-cell kinase) antagonist (IC50=1 and 20 nM in different assays). ITK antagonist inhibits insulin receptor kinase (IRK) with an IC50 of 160 nM.
| Molecular Weight | 494.65 |
| Formula | C26H34N6O2S |
| CAS Number | 1149753-56-9 |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| 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.
[4] Hua Xu, et al. ACS Chem Biol. PF-06651600, a Dual JAK3/TEC Family Kinase Inhibitor
[5] Jingjing Wu, et al. J Hematol Oncol. Second-generation inhibitors of Bruton tyrosine kinase
| Related Itk Products |
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| ITK degrader 2
ITK degrader 2 is a modulator of targeted ubiquitination and a targeted protein degrading molecule. |
| ITK degrader 1
ITK degrader 1 is a highly selective degrader of interleukin-2-inducible T-cell kinase (ITK; DC50=3.6 nM in vivo in mice). |
| PRN694
PRN694 is an irreversible, highly selective and potent covalent interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) dual inhibitor with IC50s of 0.3 nM and 1.4 nM, respectively. PRN694 exhibits extended target residence time on ITK and RLK, enabling durable attenuation of effector cells in vitro and in vivo. |
| GNE-9822
GNE-9822 is a potent, orally active and selective ITK inhibitor with a Ki value of 0.7 nM. GNE-9822 has good ADME properties. GNE-9822 can be used in research of asthma. |
| ITK inhibitor 2
ITK inhibitor 2 is a interleukin-2-inducible T-cell kinase (ITK) inhibitor, with an IC50 of 2 nM. |
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