Gsk-2250665a, an Itk inhibitor with pKi = 9.2, shows Itk selectivity against Aurora B kinase and Btk (pIC50 values 6.4 and 6.5, respectively) and a group of other kinases. Inhibit IFNγ production in PBMC.
| Molecular Weight | 459.61 |
| Formula | C26H29N5OS |
| CAS Number | 1246030-96-5 |
| 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 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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