货号	规格	价格	上海	北京	珠海	重庆	武汉
V47665-1mg	≥98%	￥2990.00 V47665-1mg ￥2990.00 3-5天	0 货期：3-5天	-	-	-	-
V47665-5mg	≥98%	￥6580.00 V47665-5mg ￥6580.00 3-5天	0 货期：3-5天	-	-	-	-
V47665-10mg	≥98%	￥10500.00 V47665-10mg ￥10500.00 3-5天	0 货期：3-5天	-	-	-	-
V47665-25mg	≥98%	￥15600.00 V47665-25mg ￥15600.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

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.

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.

参考文献：

1. Li Z, et, al. Targeted Protein Degradation Induced by HEMTACs Based on HSP90. J Med Chem. 2023 Jan 12;66(1):733-751.

保存条件：

-20°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.049 ml	5.244 ml	10.488 ml
5 mM	0.21 ml	1.049 ml	2.098 ml
10 mM	0.105 ml	0.524 ml	1.049 ml
50 mM	0.021 ml	0.105 ml	0.21 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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