| Identification | Back Directory | [Name]
Ethanone, 2-[(3,5-dichlorophenyl)amino]-1-[(2R,3R)-2-methyl-3-(7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-1-piperidinyl]- | [CAS]
1374239-71-0 | [Synonyms]
BTK-IN-18
Ethanone, 2-[(3,5-dichlorophenyl)amino]-1-[(2R,3R)-2-methyl-3-(7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-1-piperidinyl]- | [Molecular Formula]
C20H22Cl2N6O | [MOL File]
1374239-71-0.mol | [Molecular Weight]
433.33 |
| Hazard Information | Back Directory | [Uses]
BTK-IN-18 is a potent, reversible BTK inhibitor with an IC50 of 0.002 μM. BTK-IN-18 inhibits both CD69 and CD86 in vivo[1]. | [in vivo]
BTK-IN-18 (compound 41; 10, 25, 45 mg/kg; IP; single dose) causes robust dose-dependent inhibition of both CD69 and CD86[1].
BTK-IN-18 (iv; 1 mg/kg) has a T1/2 of 5.3 hours, a CL of 19 mL/min/kg, and a Vss of 1.3 L/kg for rats[1].
| Animal Model: | Mice[1] | | Dosage: | 10, 25, 45 mg/kg | | Administration: | IP; single dose | | Result: | Caused robust dose-dependent inhibition of both CD69 and CD86 (74.8 %, 50.3 %, and 21.5 % respectively).
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| Animal Model: | | | Dosage: | | | Administration: | | | Result: | Pharmacokinetic Parameters of BTK-IN-18 in rats[1].
| IV (1 mg/kg) | PO (5 mg/kg) | | Tmax (h) | | 1.6 | | Cmax (h?mg/mL) | 321 | | | AUCinfi (h?mg/mL) | 1013 | 1421 | | t1/2 (ng/mL) | 5.3 | | | CL (mL/min/kg) | 19 | | | Vss (L/kg) | 1.3 | | | F (%) | 23% | |
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| [References]
[1] George H Vandeveer, et al. Discovery of structural diverse reversible BTK inhibitors utilized to develop a novel in vivo CD69 and CD86 PK/PD mouse model. Bioorg Med Chem Lett. 2022 Dec 17;80:129108. DOI:10.1016/j.bmcl.2022.129108 |
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