2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide


CAS No. : 1258292-64-6

1258292-64-6
Price and Availability of CAS No. : 1258292-64-6
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10mg $201 In-stock
25mg $382 In-stock
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Cat. No. : HY-120469
M.Wt: 350.20
Formula: C16H13Cl2N3O2
Purity: >98 %
Solubility: DMSO : 62.5 mg/mL (ultrasonic)
Introduction of 1258292-64-6 :

GDC-046 is a potent, selective, and orally bioavailable TYK2 inhibitor with Kis of 4.8, 0.7, 0.7, and 0.4 nM for TYK2, JAK1, JAK2, and JAK3, respectively[1]. In Vitro: In cell-based assays, GDC-046 demonstrates reasonable potency in blocking the IL-12 pathway (IL-12 pSTAT4 EC50=380 nM) while displaying less activity in the EPO (JAK2) pathway (EPO pSTAT5 EC50=1700 nM) and IL-6 (JAK1) pathway (IL-6 pSTAT3 EC50=2000 nM)[1]. In Vivo: In mice, GDC-046 exhibits relatively high clearance (65 mL/min/kg) when dosed intravenously (i.v. 1 mg/kg) and exhibits modest oral exposure (AUC=2.6 μM·h at p.o. 5 mg/kg)[1].

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