OT-82 - CAS:1800487-55-1

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OT-82

目录号 : KM4668 CAS No. : 1800487-55-1 纯度 : 98%

Data Sheet 产品使用指南

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。

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5mg		In-stock
10mg		In-stock
50mg	询价	In-stock

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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.

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

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.

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.

分子式

C₂₆H₂₁FN₄O

分子量

424.47

CAS号

1800487-55-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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。
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。
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。

临床试验

纯度： 98%

Data Sheet

产品使用指南

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稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量

浓度

体积

分子量*

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

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The molarity calculator equation

The dilution calculator equation