TTT-28|cas:1609138-51-3|西域试剂

TTT-28,99.62%

产品编号：Bellancom-101511| CAS NO：1609138-51-3| 分子式：C₃₁H₃₁N₃O₆S| 分子量：573.66

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-101511		￥3500.00	杭州北京（现货）
Bellancom-101511		￥9500.00	杭州北京（现货）

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TTT-28

产品介绍

TTT-28 是一种噻唑-缬氨酸肽模拟物，高效 ABCB1 (P-gp/MDR1) 选择性抑制剂，低毒性。TTT-28 通过选择性阻断 ATP 结合盒亚家族 B 成员1 (ABCB1) 的外排功能, 逆转ABCB1介导的多药耐药性 (MDR)。

生物活性

TTT-28 is a synthesized thiazole-valine peptidomimetic, a novel selective inhibitor of ABCB1 (P-gp/MDR1) with high efficacy and low toxicity, which reverses the ATP-binding cassette sub-family B member 1 (ABCB1)-mediated multidrug resistance (MDR) by selectively blocking the efflux function of ABCB1.

体外研究

TTT-28 (0-100 μM; 72 hours) reverses ABCB1-mediated MDR in drug selected SW620/Ad300 cells and transfected HEK293/ABCB1 cells; the IC₅₀s of TTT-28 in CCD-18Co, SW620 and SW620/Ad300 cells are 213.4±11.0 μM, 89.4±3.9 μM and 92.0±5.0 μM, respectively.
TTT-28 (10 μM; 2 hours) raises the ABCB1-mediated MDR and increased the accumulation of [³H]-paclitaxel in ABCB1 overexpressing cells.
TTT-28 (10 μM; 0-72 hours) does not interfer with the expression level and localization of ABCB1, it results from blocking the efflux function of ABCB1.
TTT-28 (0-40 μM; 2 hours) interacts at the drug-substrate-binding site and actives the ATPase activity of ABCB1 in a concentration-dependent fashion.

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

Cell Viability Assay

Cell Line:	SW620 cells, SW620/Ad300 cells
Concentration:	0.1 μM, 1 μM, 10 μM, 100 μM
Incubation Time:	72 hours
Result:	Decreased the resistance fold of ABCB1 substrates (Paclitaxel, Doxorubicin, Vincristine) in SW620/Ad300 cells compared to SW620 cells.

体内研究
(In Vivo)

TTT-28 (deliver orally; 30 mg/kg; every 3 rd day; 18 days) potentiates the anticancer activity of paclitaxel due to its inhibitory effect on the efflux function of ABCB1, it enhances the inhibitory effect of paclitaxel on the growth of SW620/Ad300 tumor and promoted apoptosis.

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

Animal Model:	5-10 week Male athymic NCR (nu/nu) nude mice ABCB1 overexpressing tumor xenograft model with SW620/Ad300 cells
Dosage:	30 mg/kg
Administration:	Deliver orally; every 3rd day; 18 days
Result:	Lead to higher intratumoral accumulation of paclitaxel in tumors.

体内研究

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

Animal Model:	5-10 week Male athymic NCR (nu/nu) nude mice ABCB1 overexpressing tumor xenograft model with SW620/Ad300 cells
Dosage:	30 mg/kg
Administration:	Deliver orally; every 3rd day; 18 days
Result:	Lead to higher intratumoral accumulation of paclitaxel in tumors.

体内研究

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

Animal Model:	5-10 week Male athymic NCR (nu/nu) nude mice ABCB1 overexpressing tumor xenograft model with SW620/Ad300 cells
Dosage:	30 mg/kg
Administration:	Deliver orally; every 3rd day; 18 days
Result:	Lead to higher intratumoral accumulation of paclitaxel in tumors.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (435.80 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7432 mL	8.7160 mL	17.4319 mL
5 mM	0.3486 mL	1.7432 mL	3.4864 mL
10 mM	0.1743 mL	0.8716 mL	1.7432 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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式