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编 号：F756180
分子式：C48H53ClN16O4
分子量：953.49
分子式：C48H53ClN16O4
分子量：953.49
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CAS No: 2821803-61-4
产品详情
生物活性：
HEMTAC CDK4/6 degrader 1 is a PROTAC connected by ligands for HSP90 and CDK4/6 with a Kd value of 35.7 μM. HEMTAC CDK4/6 degrader 1 induces CDK4/6 degradation in B16F10 melanoma cells. HEMTAC CDK4/6 degrader 1 arrests cell cycle at G0/G1 phase and induces apoptosis. HEMTAC CDK4/6 degrader 1 can be used in research of cancer. HEMTAC CDK4/6 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：
HEMTAC CDK4/6 degrader 1 (compound 26; 20 and 40 mg/kg; i.p.; daily, for 15 d) has antitumor efficacy in C57BL/6J mice bearing B16F10 melanoma xenografts.Animal Model:C57BL/6J mice bearing B16F10 melanoma xenografts
Dosage:20 and 40 mg/kg
Administration:intraperitoneal injection; daily, for 15 days
Result:Inhibited tumor growth and resulted in fewer CDK4/6-positive cells and led to much more necrosis.
体外研究：
HEMTAC CDK4/6 degrader 1 (compound 26; 0.01-1 μM; 24 h) induces CDK4 and CDK6 degradation in the treated B16F10 cells with a DC50 value (the drug concentration that results in 50% protein degradation) of approximately 26 and 19 nM and a Dmax (maximal percent degradation) of 88 and 92%, respectively.HEMTAC CDK4/6 degrader 1 (0.01-100 μM; 72 h) has anti-proliferative activity against a broad range of human cancer cell lines.HEMTAC CDK4/6 degrader 1 (250 nM; 24 or 48 h) induces B16F10 cells to undergo apoptosis in a dose-dependent manner and arrests cell cycle at G0/G1 phase.
HEMTAC CDK4/6 degrader 1 is a PROTAC connected by ligands for HSP90 and CDK4/6 with a Kd value of 35.7 μM. HEMTAC CDK4/6 degrader 1 induces CDK4/6 degradation in B16F10 melanoma cells. HEMTAC CDK4/6 degrader 1 arrests cell cycle at G0/G1 phase and induces apoptosis. HEMTAC CDK4/6 degrader 1 can be used in research of cancer. HEMTAC CDK4/6 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：
HEMTAC CDK4/6 degrader 1 (compound 26; 20 and 40 mg/kg; i.p.; daily, for 15 d) has antitumor efficacy in C57BL/6J mice bearing B16F10 melanoma xenografts.Animal Model:C57BL/6J mice bearing B16F10 melanoma xenografts
Dosage:20 and 40 mg/kg
Administration:intraperitoneal injection; daily, for 15 days
Result:Inhibited tumor growth and resulted in fewer CDK4/6-positive cells and led to much more necrosis.
体外研究：
HEMTAC CDK4/6 degrader 1 (compound 26; 0.01-1 μM; 24 h) induces CDK4 and CDK6 degradation in the treated B16F10 cells with a DC50 value (the drug concentration that results in 50% protein degradation) of approximately 26 and 19 nM and a Dmax (maximal percent degradation) of 88 and 92%, respectively.HEMTAC CDK4/6 degrader 1 (0.01-100 μM; 72 h) has anti-proliferative activity against a broad range of human cancer cell lines.HEMTAC CDK4/6 degrader 1 (250 nM; 24 or 48 h) induces B16F10 cells to undergo apoptosis in a dose-dependent manner and arrests cell cycle at G0/G1 phase.
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