2445499-20-5

2445499-20-5 structure

2445499-20-5 structure

Name: JAK-IN-21
Chemical Name: JAK-IN-21
CAS Number: 2445499-20-5
Molecular Formula: C₁₉H₁₆N₈O
Molecular Weight: 372.38
Catalog: Signaling Pathways Epigenetics JAK
Create Date: 2022-11-21 13:15:22
Modify Date: 2024-01-29 19:00:46
JAK-IN-21 (Example 4) is a selective and potent JAK inhibitor with IC50s of 1.73, 2.04, 109 and 62.9 nM against JAK1, JAK2, J2V617F and TYK2, respectively[1].

Name	JAK-IN-21

Description	JAK-IN-21 (Example 4) is a selective and potent JAK inhibitor with IC50s of 1.73, 2.04, 109 and 62.9 nM against JAK1, JAK2, J2V617F and TYK2, respectively[1].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> JAK/STAT Signaling >> JAK Signaling Pathways >> Epigenetics >> JAK Signaling Pathways >> Stem Cell/Wnt >> JAK
Target	JAK1:1.73 nM (IC50) JAK2:2.04 nM (IC50) Tyk2:62.9 nM (IC50) JAK2-V617F:109 nM (IC50)
In Vitro	JAK-IN-21 (Example 4) doses not inhibit CYPs and shows good liver microsome stability[1].
In Vivo	JAK-IN-21 (Example 4) shows low bioavailability (F=1.9%)[1]. Animal Model: SD rats[1] Dosage: 10 mg/kg Administration: Oral gavage (Pharmacokinetic Study) Result: Rat Colon Pharmacokinetic Study[1] Compound Plasma Cmax (ng/mL) Plasma AUC (hng/mL) t1/2 (h) Colon AUC (hng/g) Colon + Feces AUC (hng/g) JAK-IN-21 68.8 96 1.6 6,623 545,501 Animal Model: SD rats[1] Dosage: 1 mg/kg or 2 mg/kg Administration: Intravenous injection (1 mg/kg) or oral gavage (2 mg/kg) (Pharmacokinetic Study) Result: Pharmacokinetic Parameters in Sprague-Dawley Rats by Intravenous Administration and Oral Administration[1] Compound Dose (mg/kg) AUC (hng/mL) T1/2 (h) Cl (mL/min/kg) Vd (L/kg) Cmax (ng/mL) F (%) JAK-IN-21 (iv) 1 854.8 0.22 19.4 0.37 JAK-IN-21 (ig) 2 29.8 0.38 40.4 1.9
References	[1]. Zhaokui WAN, et al. Benzamides of pyrazolyl-amino-pyrimidinyl derivatives, and compositions and methods thereof. Patent WO2020119819.

Molecular Formula	C₁₉H₁₆N₈O
Molecular Weight	372.38