TP-472|cas:2079895-62-6|西域试剂

TP-472,99.27%

产品编号：Bellancom-100517| CAS NO：2079895-62-6| 分子式：C₂₀H₁₉N₃O₂| 分子量：333.38

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-100517		￥800.00	杭州北京（现货）

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TP-472

产品介绍

TP-472 是一种选择性的 BRD9/7 抑制剂，对 BRD9 和 BRD7 作用的 K_d 值分别为 33 nM 和 340 nM。TP-472 对 BRD9 的选择性比 BRD7 以外的其他溴结构域家族成员高 30 倍以上。TP-472 诱导黑色素瘤细胞凋亡 (apoptosis)。

生物活性

TP-472 is a selective BRD9/7 inhibitor, with K_ds of 33 nM and 340 nM for BRD9 and BRD7, respectively. TP-472 exhibits >30-fold selectivity for BRD9 over other bromodomain family members except BRD7. TP-472 induces apoptosis of melanoma cells.

体外研究

TP-472 (1 µM, 3 µM; 24-216 hours) yields concentration-dependent growth defects in ESCs.
TP-472 (0.1-10 μM; 24 h) effectively inhibits the growth of both the BRAF mutant melanoma cell lines at 5 and 10 µM concentrations.
TP-472 (for 2 weeks) also strongly inhibits the long-term survival of multiple melanoma cell lines (M14, SKMEL-28, A375, and A2058) at concentrations of 5 and 10 µM.
TP-472 (5-10 μM; 24 h) treatment downregulates genes encoding various extracellular matrix (ECM) proteins, including integrins, collagens, and fibronectins in A375 cells.
TP-472 (0.1-10 μM; 24 h) results in the upregulation of pro-apoptotic genes (BAX, MDM2, CDKN1A) in A375 cells.

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

Cell Viability Assay

Cell Line:	Embryonic stem cells
Concentration:	1 µM, 3 µM
Incubation Time:	24 hours, 72 hours, 120 hours, 168 hours, 216 hours
Result:	Yields concentration-dependent growth defects in ESCs.

Cell Proliferation Assay

Cell Line:	M14 and SKMEL-28 cells
Concentration:	0.1 μM, 0.5 μM, 1 μM, 2 μM, 5 μM, 10 μM
Incubation Time:	24 h
Result:	Effectively inhibited the growth of both the BRAF mutant melanoma cell lines.

Western Blot Analysis

Cell Line:	A375 cells
Concentration:	10 μM
Incubation Time:	24 h
Result:	Resulted in the upregulation of pro-apoptotic genes.

体内研究
(In Vivo)

TP-472 (20 mg/kg; i.p.; three times a week; for 5 weeks) significantly inhibits the subcutaneous tumor growth in melanoma xenograft mouse model.

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

Animal Model:	NSG mice injected with A375-MA2 cells (male five- to six-week-old)
Dosage:	20 mg/kg
Administration:	i.p.; three times a week; for 5 weeks
Result:	Significantly inhibited the subcutaneous tumor growth in melanoma xenograft mouse model.

体内研究

TP-472 (20 mg/kg; i.p.; three times a week; for 5 weeks) significantly inhibits the subcutaneous tumor growth in melanoma xenograft mouse model.

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

Animal Model:	NSG mice injected with A375-MA2 cells (male five- to six-week-old)
Dosage:	20 mg/kg
Administration:	i.p.; three times a week; for 5 weeks
Result:	Significantly inhibited the subcutaneous tumor growth in melanoma xenograft mouse model.

体内研究

TP-472 (20 mg/kg; i.p.; three times a week; for 5 weeks) significantly inhibits the subcutaneous tumor growth in melanoma xenograft mouse model.

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

Animal Model:	NSG mice injected with A375-MA2 cells (male five- to six-week-old)
Dosage:	20 mg/kg
Administration:	i.p.; three times a week; for 5 weeks
Result:	Significantly inhibited the subcutaneous tumor growth in melanoma xenograft mouse model.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (299.96 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.9996 mL	14.9979 mL	29.9958 mL
5 mM	0.5999 mL	2.9996 mL	5.9992 mL
10 mM	0.3000 mL	1.4998 mL	2.9996 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: ≥ 2.5 mg/mL (7.50 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.50 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (7.50 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.50 mM，饱和度未知) 的澄清溶液。
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 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明