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编 号：F756058
分子式：C43H43N9O4
分子量：749.86
分子式：C43H43N9O4
分子量：749.86
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CAS No: 2801715-13-7
产品详情
生物活性：
PROTAC BTK Degrader-1 is a potent, selective and orally active PROTAC BTK degrader with an IC50 value of 34.51 nM and 64.56 nM for BTK WT and BTK-481S, respectively. PROTAC BTK Degrader-1 effectively reduces BTK protein levels and suppresses tumor growth. PROTAC BTK Degrader-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
体内研究：
PROTAC BTK Degrader-1 (compound C13) (10 and 30 mg/kg; PO, bid, for 17 days) inhibits tumor growth in the OCI-ly10 xenograft mouse model.Pharmacokinetic Parameters of PROTAC BTK Degrader-1 in ICR mice.PO (100 mg/kg) IV (2 mg/kg)
Tmax (h)1.00
T1/2 (h)8.33.7
Cmax (ng/mL)3089
AUC0-t (ng/mL·h)16,8942827
AUC0-∞ (ng/mL·h)17,0702845
VdSS (L/kg)3.1
CL (mL/min/kg)11.7
MRT (h)4.5
F (%)12
Animal Model:OCI-ly10 xenograft mouse model
Dosage:10 and 30 mg/kg
Administration:PO, bid, for 17 days
Result:Inhibited tumor growth by 50.9 and 96.9% at 10 and 30 mg/kg, respectively.
PROTAC BTK Degrader-1 is a potent, selective and orally active PROTAC BTK degrader with an IC50 value of 34.51 nM and 64.56 nM for BTK WT and BTK-481S, respectively. PROTAC BTK Degrader-1 effectively reduces BTK protein levels and suppresses tumor growth. PROTAC BTK Degrader-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
体内研究：
PROTAC BTK Degrader-1 (compound C13) (10 and 30 mg/kg; PO, bid, for 17 days) inhibits tumor growth in the OCI-ly10 xenograft mouse model.Pharmacokinetic Parameters of PROTAC BTK Degrader-1 in ICR mice.PO (100 mg/kg) IV (2 mg/kg)
Tmax (h)1.00
T1/2 (h)8.33.7
Cmax (ng/mL)3089
AUC0-t (ng/mL·h)16,8942827
AUC0-∞ (ng/mL·h)17,0702845
VdSS (L/kg)3.1
CL (mL/min/kg)11.7
MRT (h)4.5
F (%)12
Animal Model:OCI-ly10 xenograft mouse model
Dosage:10 and 30 mg/kg
Administration:PO, bid, for 17 days
Result:Inhibited tumor growth by 50.9 and 96.9% at 10 and 30 mg/kg, respectively.
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