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CAS No.: 2231744-29-7

MT-802 Catalog No. CSN22302

Synonyms: Mt-802

MT-802 (MT802) is a potent BTK PROTAC that induces degradation of both wild-type and C481S mutant BTK (DC50=9.1 nM); MT-802 recruits BTK to the cereblon E3 ubiquitin ligase complex to trigger BTK ubiquitination and degradation via the proteasome; MT-802 binds fewer off-target kinases than ibrutinib does and retains an equivalent potency (>99% degradation at nanomolar concentrations) against wild-type and C481S BTK, elicits complete BTK knockdown at 250 nM; reduces the pool of active, phosphorylated BTK in cells isolated from CLL patients with the C481S mutation, whereas ibrutinib cannot.

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400-920-2911

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技术信息

生物活性

描述MT-802 is a potent BTK PROTAC that induces degradation of both wild-type and C481S mutant BTK (DC50=9.1 nM). MT-802 recruits BTK to the cereblon E3 ubiquitin ligase complex to trigger BTK ubiquitination and degradation via the proteasome. MT-802 binds fewer off-target kinases than ibrutinib does and retains an equivalent potency (>99% degradation at nanomolar concentrations) against wild-type and C481S BTK. In cells isolated from CLL (chronic lymphocytic leukemia) patients with the C481S mutation, MT-802 is able to reduce the pool of active, phosphorylated BTK whereas ibrutinib cannot^[1].
参考文献

[1] Buhimschi AD, Armstrong HA, Toure M, Jaime-Figueroa S, Chen TL, Lehman AM, Woyach JA, Johnson AJ, Byrd JC, Crews CM. Targeting the C481S Ibrutinib-Resistance Mutation in Bruton's Tyrosine Kinase Using PROTAC-Mediated Degradation. Biochemistry. 2018 Jul 3;57(26):3564-3575.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.2693 mL
- 6.3466 mL
- 12.6933 mL
- 5 mM
- 0.2539 mL
- 1.2693 mL
- 2.5387 mL
- 10 mM
- 0.1269 mL
- 0.6347 mL
- 1.2693 mL

技术信息

CAS号	2231744-29-7	储存条件	粉末 Keep in dark place,Inert atmosphere,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C41H41N9O8	运输	蓝冰
分子量	787.82	别名	Mt-802

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