OT-82|cas:1800487-55-1|西域试剂

OT-82,99.84%

产品编号：Bellancom-136241| CAS NO：1800487-55-1| 分子式：C₂₆H₂₁FN₄O| 分子量：424.47

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货号	价格	库存与货期
Bellancom-136241	￥2700.00	杭州北京（现货）
Bellancom-136241	￥4350.00	杭州北京（现货）
Bellancom-136241	￥13950.00	杭州北京（现货）

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OT-82

产品介绍

OT-82 是一种强效、选择性和具有口服活性的 NAMPT 的抑制剂。OT-82 对造血源细胞有选择性毒性，以 NAD⁺依赖方式诱导细胞死亡。OT-82 是一种很有前途的抗肿瘤试剂 (antineoplastic agent)，用于血液系统恶性肿瘤的研究。

生物活性

OT-82 is a potent, selective and orally active inhibitor of NAMPT. OT-82 is selectively toxic to cells of hematopoietic origin and induces cell death in a NAD⁺ dependent manner. OT-82 is a promising antineoplastic agent for the study of hematological malignancies.

体外研究

OT-82 (0.0001-10 μM; 72 hours) demonstrates tissue-selective (HP vs non-HP) cytotoxicity. It is against HP cell lines MV4–11, U937, RS4;11, HEL92.1.7 and PER485 cell growth with IC₅₀ values of 2.11 nM, 2.70 nM, 1.05 nM and 1.36 nM, respectively. It also against nonHP cell lines MCF-7, U87, HT29, and H1299 cell growth with IC₅₀ values of 37.92 nM, 29.52 nM, 15.67 nM and 7.95 nM , respectively.
OT-82 demonstrates cancer-selective (tumor vs normal) cytotoxicity. It more sensitive to BMMNC from leukemia patients, the IC₅₀ values are 31 nM and 7.10 nM for AML and ALL donors, respectively. The IC₅₀ value is 62.69 nM for BMMNC from healthy donors.
OT-82 (0.001-10 μM; 48 hours) inhibits recombinant NAMPT activity and causes dose-dependent reductions in cellular NAD and ATP concentrations in MV4–11 cells.
OT-82 (0.01-100 nM; 48 hours) results in activation of caspase-3, an increase in the proportion of cells with sub-G1 DNA content, and depolarization of the mitochondrial membrane in MV4–11 cells.

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

Cell Viability Assay

Cell Line:	HP cell lines (MV4–11, U937, RS4;11, HEL92.1.7, PER485) Non-HP cell lines (MCF-7, U87, HT29, H1299)
Concentration:	0.0001 μM-10 μM
Incubation Time:	72 hours
Result:	Was against human cell lines derived from hematological malignancies (HP) with IC₅₀ values ranging from 1.10 nM to 5.86 nM, and was against non-HP cancers with IC₅₀ ranging from 1.10 nM to 37.92 nM.

Apoptosis Analysis

Cell Line:	MV4–11 cells
Concentration:	0.01-100 nM
Incubation Time:	48 hours
Result:	Exhibited hallmarks of apoptotic cell death

体内研究
(In Vivo)

OT-82 (oral gavage; 20 or 40 mg/kg; 3 weeks) treatment increases survival to 100% and 56% at 40 or 20 mg/kg, respectively after treatment discontinuation in SC xenograft model of Burkitt's lymphoma.

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

Animal Model:	SC xenograft model of Burkitt's lymphoma in SCID mice
Dosage:	20 or 40 mg/kg
Administration:	oral gavage; 3 weeks
Result:	Potently inhibited tumor growth of multiple myeloma mouse model.

体内研究

OT-82 (oral gavage; 20 or 40 mg/kg; 3 weeks) treatment increases survival to 100% and 56% at 40 or 20 mg/kg, respectively after treatment discontinuation in SC xenograft model of Burkitt's lymphoma.

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

Animal Model:	SC xenograft model of Burkitt's lymphoma in SCID mice
Dosage:	20 or 40 mg/kg
Administration:	oral gavage; 3 weeks
Result:	Potently inhibited tumor growth of multiple myeloma mouse model.

体内研究

OT-82 (oral gavage; 20 or 40 mg/kg; 3 weeks) treatment increases survival to 100% and 56% at 40 or 20 mg/kg, respectively after treatment discontinuation in SC xenograft model of Burkitt's lymphoma.

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

Animal Model:	SC xenograft model of Burkitt's lymphoma in SCID mice
Dosage:	20 or 40 mg/kg
Administration:	oral gavage; 3 weeks
Result:	Potently inhibited tumor growth of multiple myeloma mouse model.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (235.59 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3559 mL	11.7794 mL	23.5588 mL
5 mM	0.4712 mL	2.3559 mL	4.7118 mL
10 mM	0.2356 mL	1.1779 mL	2.3559 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: ≥ 2.08 mg/mL (4.90 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.90 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (4.90 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.90 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.90 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.90 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。