2. PROTAC Epigenetics
  3. PROTACs Epigenetic Reader Domain
  4. XYD270

XYD270 是一种口服有效的 BRD9 PROTAC 降解剂。XYD270 可抑制癌细胞增殖。XYD270 在急性髓系白血病小鼠模型中抑制肿瘤生长。XYD270 可用于滑膜肉瘤、急性髓系白血病的相关研究。

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XYD270

XYD270 Chemical Structure

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XYD270 相关抗体

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

XYD270 is an orally active BRD9 PROTAC degrader. XYD270 inhibits the proliferation of cancer cells. XYD270 suppresses tumor growth in a mouse model of acute myeloid leukemia. XYD270 can be used in research related to synovial sarcoma and acute myeloid leukemia[1].

IC50 & Target[1]

Cereblon

 

BRD9

 

体外研究
(In Vitro)

XYD270 (Compound 32) (0-500 nM, 24 h) 可强效且选择性地降解 HS-SY-II、MV4;11 细胞中的 BRD9，DC50 分别为 0.082、3.9 nM，Dmax 分别为 96%、90%[1]。
XYD270 (0.0001-100 μM; 96 h) 可强效抑制 HS-SY-II 滑膜肉瘤细胞 (IC50 = 1.65 μM) 和 MV4;11 急性髓系白血病细胞 (IC50 = 0.05 μM) 的增殖，并抑制 HS-SY-II 细胞的长期集落形成[1]。

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

XYD270 相关抗体:

Western Blot Analysis[1]

Cell Line: HS-SY-II synovial sarcoma cells
Concentration: 0, 0.03, 0.16, 0.8, 4, 20, 100, 500 nM
Incubation Time: 24 h
Result: Induced potent, concentration-dependent BRD9 degradation with a DC50 of 0.082 nM and a maximal degradation (Dₘₐₓ) of 96%.
Achieved significant BRD9 degradation (89%) within 0.5 h of treatment with 10 nM.
Did not reduce protein levels of BRD4, BRD7, or CRBN neo-substrates (GSPT1, IKZF1, CK1α).
Confirmed significant BRD9 downregulation with no significant changes in homologous bromodomain proteins or CRBN neo-substrates via label-free quantitative proteomic profiling.

Western Blot Analysis[1]

Cell Line: MV4;11 acute myeloid leukemia cells
Concentration: 0, 0.03, 0.16, 0.8, 4, 20, 100, 500 nM
Incubation Time: 24 h
Result: Induced concentration-dependent BRD9 degradation with a DC50 of 3.9 nM and a Dₘₐₓ of 90%.
Did not induce degradation of CRBN neo-substrates (GSPT1, IKZF1, CK1α).
Confirmed significant BRD9 downregulation with no significant changes in homologous bromodomain proteins or CRBN neo-substrates via label-free quantitative proteomic profiling.

Cell Proliferation Assay[1]

Cell Line: HS-SY-II synovial sarcoma cells, MV4;11 acute myeloid leukemia cells
Concentration: 0.0001, 0.01, 1, 100 μM
Incubation Time: 96 h
Result: Inhibited HS-SY-II cell proliferation with an IC50 of 1.65 μM, and MV4;11 cell proliferation with an IC50 of 0.05 μM.
Inhibited HS-SY-II colony formation in a concentration-dependent manner with superior efficacy compared to dBRD9.
体内研究
(In Vivo)

XYD270 (10 mg/kg；口服；每日 1 次；28 天) 在 BALB/c-Nude 小鼠的 MV4;11 AML 异种移植模型中可实现 54%的肿瘤生长抑制，且未出现显著的体重下降[1]。

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

Animal Model: BALB/c-Nude (male, 5 weeks old, subcutaneous inoculation with MV4;11 cells)[1]
Dosage: 10 mg/kg
Administration: p.o.; once daily; 28 days
Result: Achieved a tumor growth inhibition (TGI) rate of 54%.
Showed no significant reduction in body weight.
分子量

692.85

Formula

C40H48N6O5
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

XYD270 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

XYD270XYD 270XYD-270PROTACsEpigenetic Reader DomainBRD9 PROTAC degraderHS-SY-II cellsMV4;11 cellsBALB/c-Nude micesynovial sarcomaacute myeloid leukemiaInhibitorinhibitorinhibit

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目录号：
HY-182082
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