2. Epigenetics PROTAC
  3. Histone Acetyltransferase PROTACs
  4. CBPD-409

CBPD-409 是一种口服有效的 CBP/p300 降解剂，DC50 为 0.2–0.4 nM。CBPD-409 在 AR+ 前列腺癌细胞系 VCaP、LNCaP 和 22Rv1 中表现出抗增殖作用，IC50 为 1.2–2.0 nM。CBPD-409 具有抗肿瘤活性 (Red: CBP inhibitor GNE049 (HY-108435); Blue: CRBN/cullin 4A Thalidomide (HY-14658); Black: Linker)。

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CBPD-409 Chemical Structure

CBPD-409 Chemical Structure

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CBPD-409 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

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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

CBPD-409 is an orally active PROTAC degrader for CBP/p300, with DC50 of 0.2–0.4 nM. CBPD-409 exhibits antiproliferative effects in AR+ prostate cancer cell lines VCaP, LNCaP and 22Rv1, with IC50s of 1.2–2.0 nM. CBPD-409 exhibits antitumor efficacy (Red: CBP inhibitor GNE049 (HY-108435); Blue: CRBN/cullin 4A Thalidomide (HY-14658); Black: Linker)[1].

体外研究
(In Vitro)

CBPD-409 (0.01-10 nM) 抑制前列腺癌细胞 VCaP，LNCaP 和 22Rv1 中的 AR 信号转导和 c-Myc 表达[1]。

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

CBPD-409 相关抗体:

RT-PCR[1]

Cell Line: VCaP, LNCaP and 22Rv1
Concentration: 0.01-10 nM
Incubation Time: 6 h
Result: Reduced mRNA levels of KLK3, AR and c-Myc.
体内研究
(In Vivo)

CBPD-409 (1 mg/kg，静脉注射；3 mg/kg，口服) 在 ICR 小鼠模型中的清除率 CL 为 1.7 mL/min/kg，半衰期为 T1/2 为 2.8 小时 (静脉注射) 和 2.6 小时 (口服)，血药浓度 Cmax 为 2494 ng/mL，口服生物利用度 F=50%[1]。
CBPD-409 (0.3-1 mg/kg，口服，每天一次共 5 周) 对 VCaP 前列腺癌具有抗肿瘤活性，肿瘤生长抑制率 TGI 为 73-87%，在 VCaP 异种移植小鼠模型中没有明显毒性[1]。

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

Animal Model: VCaP xenograft CB17 SCID mice model[1]
Dosage: 0.3-1 mg/kg
Administration: p.o., once a day for 5 weeks
Result: Inhibited tumor growth with TGI of 73% (0.3 mg/kg) and 87% (1 mg/kg), without significant body weight loss.
分子量

862.97

Formula

C46H52F2N10O5
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

CBPD-409 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 *
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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:

CBPD-409CBPD409CBPD 409Histone AcetyltransferasePROTACsHATsHATVCaPLNCaP22Rv1CB17 SCID miceICR miceorally activeInhibitorinhibitorinhibit

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产品名称：
CBPD-409
目录号：
HY-158113
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