Bromosporine|cas:1619994-69-2|西域试剂

Bromosporine,99.69%

产品编号：Bellancom-15815| CAS NO：1619994-69-2| 分子式：C₁₇H₂₀N₆O₄S| 分子量：404.44

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货号	价格	库存与货期
Bellancom-15815	￥1082.00	杭州北京（现货）
Bellancom-15815	￥1925.00	杭州北京（现货）
Bellancom-15815	￥7149.00	杭州北京（现货）

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Bromosporine

产品介绍

Bromosporine 是一种有效的 BET 抑制剂，对 PCAF 的 IC₅₀ 为 2.1 μM。Bromosporine 能阻滞癌细胞的细胞周期，诱导细胞凋亡 (apoptosis)。Bromosporine 与 5-FU (HY-90006) 联合使用时，在移植瘤小鼠模型中表现出良好的抗肿瘤活性。在 HIV-1 潜伏期模型中，Bromosporine 可增加 CDK9 T-loop 磷酸化，从而保护 HIV-1 复制免受潜伏期的影响。Bromosporine 可用于大肠癌、急性髓系白血病 (AML) 和艾滋病 (AIDS) 的研究。

生物活性

Bromosporine is a potent BET inhibitor with an IC₅₀ value of 2.1 μM for PCAF. Bromosporine can arrest cell cycle and induce apoptosis in cancer cells. Bromosporine exhibits excellent antitumor activity in xenograft mice model when combined with 5-FU (HY-90006). Bromosporine can increase CDK9 T-loop phosphorylation in HIV-1 latency models, resulting the protection of reactivate HIV-1 replication from latency. Bromosporine can be used to research colorectal cancer, acute myeloid leukemia (AML) and AIDS^[4].

体外研究

Bromosporine (0-1000 nM; 72 h) synergistically inhibits cell growth in CRC cells with 5-FU (HY-90006).
Bromosporine (various concentration; 48 h) causes a distinct increase in the cells arrested at G1 phase when combined with 5-FU.
Bromosporine (various concentration; 48 h) decreases the expressions of PARP, caspase 3, and 9.
Bromosporine (0.1, 0.5 and 1 μM; 6-10 days) inhibits AML cells in a dose-dependent manner.
Bromosporine (2.5 μM; 72 h) activates HIV-1 replication in vitro in latent HIV-1 J-Lat clone C11 cells^[4].
Bromosporine (1-50 μM; 48 h) does not induce marked toxicity in primary CD4+ T cells^[4].

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

Cell Proliferation Assay

Cell Line:	HCT116 and HT29
Concentration:	0, 30, 60, 120, 240, 480 and 1000 nM
Incubation Time:	72 h
Result:	Synergistically inhibited cell growth in CRC cells with 5-FU (HY-90006) (0-16 μg/mL) and exhibited a dose-dependent manner.

Cell Cycle Analysis

Cell Line:	HCT116 and HT29
Concentration:	Various concentration
Incubation Time:	48 h
Result:	Caused a distinct increase in the cells arrested at G1 phase when combined with 5-FU (HY-90006).

Western Blot Analysis

Cell Line:	HCT116 and HT29
Concentration:	Various concentration
Incubation Time:	48 h
Result:	Elevated the level of apoptosis in both cell lines through cleavage of PARP, caspase 3, and 9.

Cell Proliferation Assay

Cell Line:	MV4;11, KASUMI-1, OCI-AML3 and K562
Concentration:	0.1, 0.5 and 1 μM
Incubation Time:	6-10 days
Result:	Inhibited these AML cells in a dose-dependent manner.

Cell Cytotoxicity Assay^[4]

Cell Line:	PBMCs
Concentration:	1 μM, 2.5 μM, 5 μM, 10 μM, 25 μM and 50 μM
Incubation Time:	48 h
Result:	Did not induce marked toxicity in primary CD4+ T cells with CC₅₀ over 10 μM.

体内研究
(In Vivo)

Bromosporine (100 mg/kg; i.p.; daily for 10 days) shows better antitumor activity than individual when co-treated with 5-FU (HY-90006).

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

Animal Model:	Female BALB/c nude mice (5-6 weeks; injected with 1 × 10⁶ cells/100 μL of HT116 cells)
Dosage:	100 mg/kg
Administration:	i.p.; daily for 10 days
Result:	Exhibited better antitumor activity than individual Bromosporine or 5-FU (HY-90006) when co-treated with the two agent.

体内研究

Bromosporine (100 mg/kg; i.p.; daily for 10 days) shows better antitumor activity than individual when co-treated with 5-FU (HY-90006).

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

Animal Model:	Female BALB/c nude mice (5-6 weeks; injected with 1 × 10⁶ cells/100 μL of HT116 cells)
Dosage:	100 mg/kg
Administration:	i.p.; daily for 10 days
Result:	Exhibited better antitumor activity than individual Bromosporine or 5-FU (HY-90006) when co-treated with the two agent.

体内研究

Bromosporine (100 mg/kg; i.p.; daily for 10 days) shows better antitumor activity than individual when co-treated with 5-FU (HY-90006).

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

Animal Model:	Female BALB/c nude mice (5-6 weeks; injected with 1 × 10⁶ cells/100 μL of HT116 cells)
Dosage:	100 mg/kg
Administration:	i.p.; daily for 10 days
Result:	Exhibited better antitumor activity than individual Bromosporine or 5-FU (HY-90006) when co-treated with the two agent.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 51.7 mg/mL (127.83 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4726 mL	12.3628 mL	24.7255 mL
5 mM	0.4945 mL	2.4726 mL	4.9451 mL
10 mM	0.2473 mL	1.2363 mL	2.4726 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 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.18 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。