Inobrodib CCS1477|cas:2222941-37-7|西域试剂

Inobrodib CCS1477,99.42%

产品编号：Bellancom-111784| CAS NO：2222941-37-7| 分子式：C₃₀H₃₂F₂N₄O₃| 分子量：534.60

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-111784	￥1900.00	杭州北京（现货）
Bellancom-111784	￥3400.00	杭州北京（现货）
Bellancom-111784	￥7200.00	杭州北京（现货）
Bellancom-111784	￥10200.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

Inobrodib CCS1477

产品介绍

Inobrodib (CCS1477) 是一种口服活性的、有效且选择性强的 p300/CBP 抑制剂。Inobrodib 与 p300 和 CBP 结合，K_d 值为 1.3 和 1.7 nM，与 K_d 为 222 nM 的 BRD4 相比，具有 170/130 倍的选择性。Inobrodib 抑制前列腺癌细胞系的细胞增殖并降低雄激素受体 (AR) 和 C-MYC 调节的基因表达。

生物活性

Inobrodib (CCS1477) is an orally active, potent, and selective inhibitor of the p300/CBP bromodomain. Inobrodib binds to p300 and CBP with K_d values of 1.3 and 1.7 nM, respectively, and with 170/130-fold selectivity compared with BRD4 with a K_d of 222 nM. CCS1477 inhibits cell proliferation in prostate cancer cell lines and decreases androgen receptor (AR)- and C-MYC-regulated gene expression.

体外研究

Inobrodib binding to cellular histones in an in-cell BRET assay gives an IC50 of 19 nM for p300 and 1,060 nM for BRD4. Inobrodib shows potent growth-inhibitory activity in VCaP, 22Rv1, and LNCaP95 (all IC50 < 100 nM) that express both AR-FL and AR-V7.
Inobrodib (0-3000 nM; 48 hours) reduces expression of AR-regulated genes (KLK2, KLK3, and TMPRSS2) in both 22Rv1 and LNCaP95 cells. Inobrodib also reduces C-MYC protein expression in both 22Rv1 and LNCaP95 cells and AR-V7 protein expression in 22Rv1 cells, without clear impact on AR-FL protein expression in 22Rv1 and LNCaP95 cells. Inobrodib reduces C-MYC mRNA and downstream AR and C-MYC signaling in 22Rv1 and C4-2 cells at 16 hours. Inobrodib regulates AR signaling by affecting the recruitment of CBP, p300, and AR-FL to known AR binding sites, and has the potential to abrogate persistent AR signaling in CRPC.

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

体内研究

Inobrodib (10-30 mg/kg; oral gavage; 10 or 20 mg/kg daily (QD) or 30 mg/kg every other day (QOD) for 28 days) suppresses growth of a 22Rv1 mouse xenograft model with associated reduction in AR signaling.
Inobrodib (20 mg/kg; oral gavage; daily for 8 days) decreases AR and AR-V7 signaling and inhibits growth in a patient- derived model of lethal prostate cancer (NOD/SCID gamma (NSG) male castrated mice).

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

Animal Model:	Noncastrated male athymic nude mice
Dosage:	10-30 mg/kg
Administration:	Oral gavage; at 10 or 20 mg/kg daily (QD) or at 30 mg/kg every other day (QOD) for 28 days
Result:	Affected tumor growth at 10 mg/kg daily, 20 mg/kg daily, and 30 mg/kg every other day.

体内研究

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

Animal Model:	Noncastrated male athymic nude mice
Dosage:	10-30 mg/kg
Administration:	Oral gavage; at 10 or 20 mg/kg daily (QD) or at 30 mg/kg every other day (QOD) for 28 days
Result:	Affected tumor growth at 10 mg/kg daily, 20 mg/kg daily, and 30 mg/kg every other day.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (187.06 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8706 mL	9.3528 mL	18.7056 mL
5 mM	0.3741 mL	1.8706 mL	3.7411 mL
10 mM	0.1871 mL	0.9353 mL	1.8706 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 5.25 mg/mL (9.82 mM); Clear solution

此方案可获得 ≥ 5.25 mg/mL (9.82 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 52.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 5.25 mg/mL (9.82 mM); Clear solution

此方案可获得 ≥ 5.25 mg/mL (9.82 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 52.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
3.

请依序添加每种溶剂： 5% DMSO 40% PEG300 5% Tween-80 50% saline
Solubility: ≥ 2.5 mg/mL (4.68 mM); Clear solution
4.

请依序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (4.68 mM); Clear solution