2. PROTAC Epigenetics
  3. PROTACs Histone Acetyltransferase
  4. PROTAC KAT2A/B degrader-1

PROTAC KAT2A/B degrader-1 是一种具有口服活性的组蛋白乙酰转移酶 KAT2A/KAT2B PROTAC 降解剂。PROTAC KAT2A/B degrader-1 可诱导 KAT2A 和 KAT2B 蛋白降解。PROTAC KAT2A/B degrader-1 可抑制急性髓系白血病和小细胞肺癌细胞的增殖。PROTAC KAT2A/B degrader-1 可用于急性髓系白血病、小细胞肺癌的相关研究。

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PROTAC KAT2A/B degrader-1

PROTAC KAT2A/B degrader-1 Chemical Structure

CAS No. : 3031606-85-3

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PROTAC KAT2A/B degrader-1 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC KAT2A/B degrader-1 is an orally active histone acetyltransferase KAT2A/KAT2B PROTAC degrader. PROTAC KAT2A/B degrader-1 induces degradation of KAT2A and KAT2B proteins. PROTAC KAT2A/B degrader-1 inhibits proliferation of acute myeloid leukemia and small cell lung cancer cells. PROTAC KAT2A/B degrader-1 can be used for the research of acute myeloid leukemia, small cell lung cance[1].

体外研究
(In Vitro)

PROTAC KAT2A/B degrader-1 (Compound 24) 可在 MOLM-13 急性髓系白血病 (AML) 细胞中强效降解 KAT2A，其 DC50 为 1.53 nM，最大降解率达 90%[1]。
PROTAC KAT2A/B degrader-1 可在 NCI-H1048 SCLC 细胞中强效降解 KAT2A (DC50 = 1.39 nM, Dmax = 95%) 和 KAT2B (DC50 16.5 nM)[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

PROTAC KAT2A/B degrader-1 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route CL T1/2 Vd F AUC Cmax
Mice[1] 1 mg/kg i.v. 1.0 mL/min/kg 5.3 h 0.4 L/kg / / /
Mice[1] 1 mg/kg p.o. / / / 47 % 101.3 nM·h 10.4 nM
体内研究
(In Vivo)

PROTAC KAT2A/B degrader-1 (Compound 24) (1-50 mg/kg；口服；单剂量) 在 50 mg/kg 剂量下可使 CD-1 小鼠游离血浆浓度达到并维持在 H1048 KAT2A DC90 阈值 (22 nM) 以上至少 24 小时[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: CD-1 mice[1]
Dosage: 1 mg/kg; 50 mg/kg
Administration: P.o.; single dose
Result: Reached a peak free plasma concentration of ~0.01 μM and remained above the H1048 KAT2A DC50 threshold (1.39 nM) through 8 hours, declining thereafter (1 mg/kg dose).
Reached a peak free plasma concentration of ~0.4 μM, remained above the H1048 KAT2A DC90 threshold (22 nM) for at least 24 hours, and demonstrated proportional increases in exposure relative to the 1 mg/kg dose (50 mg/kg dose).
分子量

619.07

Formula

C31H31ClN6O6
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

PROTAC KAT2A/B degrader-1 相关分类

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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PROTAC KAT2A/B degrader-13031606-85-3PROTACsHistone AcetyltransferaseHATsHATneuroendocrine prostate cancerMOLM-13 AML cellsNCI-H1048 SCLC cellsacute myeloid leukemiasmall cell lung cancerCD-1 miceKAT2BKAT2AInhibitorinhibitorinhibit

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