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 (Structure 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

CAS No. : 2832961-58-5

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1 mg ￥3900
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CBPD-268 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

查看所有亚型
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 Histone Acetyltransferase 亚型特异性产品:

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CBP/p300 GCN5/PCAF TIP60 MOZ/MORF HBO1

  • 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 (Structure 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 DC50 值分别为 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
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

CBPD-268 相关分类

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  • 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-2682832961-58-5CBPD268CBPD 268PROTACsHistone AcetyltransferaseHATsHATorally activeprostate cancer22Rv1LNCaPVCaP cellsInhibitorinhibitorinhibit

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目录号：
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