2. PROTAC Epigenetics
  3. PROTACs Histone Acetyltransferase
  4. CBPD-268

CBPD-268 是一种有效的具有口服活性的 CBP/p300 PROTAC 降解剂，DC50 值为 ≤ 0.03 nM。CBPD-268 诱导 CBP/p300 降解并抑制细胞生长。CBPD-268 显示出抗肿瘤活性。CBPD-268 具有研究 AR 阳性前列腺癌的潜力 (Srtucture Note: Red, Androgen receptor degrader (HY-W248665A); Blue, CBP/p300 ligand (HY-161483); Black, Linker)。

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CBPD-268 Chemical Structure

CBPD-268 Chemical Structure

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CBPD-268 相关抗体

Top Publications Citing Use of Products

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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-268 is a potent and orally active CBP/p300 PROTAC degrader with an DC50 value of ≤ 0.03 nM. CBPD-268 induces CBP/p300 degradation and inhibits cell growth. CBPD-268 shows antitumor activity. CBPD-268 has the potential for the research of AR-positive prostate cancer (Srtucture Note: Red, Androgen receptor degrader (HY-W248665A); Blue, CBP/p300 ligand (HY-161483); Black, Linker)[1].

体外研究
(In Vitro)

CBPD-268 (4, 24 h) 在 22Rv1 细胞中对 CBP 和 p300 蛋白显示出高降解效率，4 小时时 DC50s 为 0.01、0.03 nM[1].
CBPD-268 通过与 CBP/p300 和 CRBN 蛋白结合而显示出降解作用[1]。
CBPD-268 (0-1000 nM; 4 days) 抑制细胞生长，对 22Rv1、LNCaP、VCaP 细胞的 IC50 值分别为 3.7、10.3、4.6 nM [1]。

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

CBPD-268 相关抗体:

Cell Viability Assay[1]

Cell Line: 22Rv1, LNCaP, VCaP cells
Concentration: 0-1000 nM
Incubation Time: 4 days
Result: Inhibited cell growth with IC50s OF 3.7, 10.3, 4.6 Nm for 22Rv1, LNCaP, VCaP cells, respectively.
体内研究
(In Vivo)

CBPD-268 (0.3, 1, 3, 10, 30 mg/kg; p.o.; once) 单次口服 0.3-3 mg/kg 可诱导肿瘤组织中 CBP 和 p300 蛋白的降解[1].
CBPD-268 (1, 3 mg/kg; p.o.; twice a week for 1 mg/kg or 3 mg/kg weekly for 4-weeks) 显示出抗肿瘤活性[1]。
药代动力学分析[1].

Species IV (mg/kg) T1/2 (h) V1/2(L/kg) CL (mL/min/kg) PO(mg/kg) T1/2 (h) Cmax (ng/ml) AUC(h*ng/mL) F(%)
Rats 1 1.9 4.9 34.6 3 1.3 220.6 936.9 67
Mice 1 3.4 1.6 6.0 3 3.1 724.7 4190.4 60

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

Animal Model: male CB17 SCID mice (VCaP xenograft tumor)[1]
Dosage: 0.3, 1, 3, 10, 30 mg/kg
Administration: P.o.; once
Result: Induced depletion of both CBP and p300 proteins in the VCaP tumor tissue in a dose-dependent manner.
Animal Model: male CB17 SCID mice (VCaP xenograft tumor model)[1]
Dosage: 1, 3 mg/kg
Administration: P.o.; twice a week for 1 mg/kg or 3 mg/kg weekly for 4-weeks
Result: Inhibited tumor growth and shows little effect on animal body weight.
Animal Model: female BALB/c mice[1]
Dosage: 3, 10, 30 mg/kg
Administration: P.o.; twice weekly for 5-6 weeks
Result: Induced no weight loss or other signs of toxicity at both 3 and 10 mg/kg dose-levels in both male and female mice.
Animal Model: Female Sprague–Dawley (SD) rats[1]
Dosage: 1-10 mg/kg
Administration: P.o.; twice a week for 5 weeks
Result: Did not cause animal body weight loss during the entire experiment and did not induce any signs of toxicity during the entire experiment.
分子量

819.90

Formula

C44H47F2N9O5
Unlabeled Cas

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-268 相关分类

  • 摩尔计算器

  • 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:

CBPD-268CBPD268CBPD 268PROTACsHistone AcetyltransferaseHATsHATorally activeprostate cancer22Rv1LNCaPVCaP cellsInhibitorinhibitorinhibit

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目录号：
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