RBN-2397

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

RBN-2397  纯度: 99.45%

RBN-2397 是一种强效的,跨物种的,且具有口服活性的 NAD+ 竞争性 PARP7 抑制剂,IC50 值小于 3 nM。RBN-2397 有选择性地结合 PARP7 (Kd=0.001 μM) 并可以恢复干扰素 I 型信号转导。RBN-2397 有潜力用于研究晚期或转移性实体肿瘤。

RBN-2397

RBN-2397 Chemical Structure

CAS No. : 2381037-82-5

规格 价格 是否有货 数量
5 mg ¥5000 In-stock
10 mg ¥8500 In-stock
25 mg ¥12500 In-stock
50 mg 询价
100 mg 询价

* Please select Quantity before adding items.

RBN-2397 相关产品

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  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Epigenetics Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Anti-Aging Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Targeted Diversity Library

生物活性

RBN-2397 is a potent, accross species and orally active NAD+ competitive inhibitor of PARP7 (IC50<3 nm). rbn-2397 selectively binds to parp7 (Kd=0.001 μM) and restores IFN signaling. RBN-2397 has the potential for the study of advanced or metastatic solid tumors[1][2].

IC50 & Target[2]

PARP-7

3 nM (IC50)

PARP-7

1 nM (Kd)

体外研究
(In Vitro)

RBN-2397 (0.0001-100 μM; 24 hours) inhibits cells proliferation with an IC50 value of 20 nM in NCI-H1373 lung cancer cells[2].
RBN-2397 (0.4 nM-1 μM; 24 hours) shows a restoration of type I IFN response by an increase in STAT1 phosphorylation as a dose-dependent manner in NCI-H1373 human lung cancer cells[2].
RBN-2397 (0.0001-1 μM; 24 hours) inhibits cell MARylation in a cell biochemial assay with an EC50 value of 1 nM[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[2]

Cell Line: NCI-H1373 lung cancer cells
Concentration: 0.0001 μM; 0.001 μM; 0.001 μM; 0.1 μM; 1 μM; 10 μM; 100 μM
Incubation Time: 24 hours
Result: Blocked cell proliferation.

Western Blot Analysis[2]

Cell Line: NCI-H1373 lung cancer cells
Concentration: 0.4 nM-1 μM
Incubation Time: 24 hours
Result: Increased p-STAT1 protein expression.

体内研究
(In Vivo)

RBN-2397 (oral administration; 3-100 mg/kg; once daily; 24-32 days) induces tumor-specific adaptive immune memory in CT26 syngeneic model with durable complete responses in CT26 tumor-bearing BALB/c mice[2].
RBN-2397 (oral administration; 3-100 mg/kg; once daily; 32 days) causes complete regressions at the dose 100 mg/kg and exerts a dose-dependent effects on tumor growth at dose levels of ≥30 mg/kg[2].
The half-life (t1/2) of RBN-2397 in vivo is 325 mins[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: CB17 SCID mice with NCI-H1373 xenografts[2]
Dosage: 3 mg/kg, 10mg/kg, 30 mg/kg, 100 mg/kg
Administration: Oral administration; once daily; 24-32 days
Result: Decreased tumor volume and exerted anti-tumor effects.

Clinical Trial

分子量

523.43

Formula

C20H23F6N7O3

CAS 号

2381037-82-5

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 : 200 mg/mL (382.10 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9105 mL 9.5524 mL 19.1048 mL
5 mM 0.3821 mL 1.9105 mL 3.8210 mL
10 mM 0.1910 mL 0.9552 mL 1.9105 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: 5% DMSO    95% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.78 mM); Clear solution

  • 2.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.97 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.97 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

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.97 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.97 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
  • 4.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.97 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.97 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。

  • 5.

    请依序添加每种溶剂: 1% DMSO    99% saline

    Solubility: ≥ 0.5 mg/mL (0.96 mM); Clear solution

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. RBN-2397-Inhibiting PARP7, a Key monoPARP Cancer Dependency

    [2]. Melissa Vasbinder, et al. RBN-2397: A First-in-Class PARP7 Inhibitor Targeting a Newly Discovered Cancer Vulnerability in Stress-Signaling Pathways.

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RBN013209

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

RBN013209 

RBN013209 是一种有效的 CD38 抑制剂,可用于癌症治疗。

RBN013209

RBN013209 Chemical Structure

CAS No. : 2597933-17-8

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100 mg   询价  
250 mg   询价  
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生物活性

RBN013209 is a potent CD38 inhibitor and is useful in the treatment of cancer.

分子量

384.43

Formula

C19H24N6O3

CAS 号

2597933-17-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Laurie B. Schenkel, et al. Heterobicyclic amides as inhibitors of cd38. WO2021021986 A1.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

RBN012759

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

RBN012759  纯度: 99.88%

RBN012759 是一种有效的,选择性和具有口服活性的 PARP14 抑制剂,IC50 值 <3 nM,比对 monoPARPs 的选择性高 300 倍,比对 polyPARPs 的选择性高 1000 倍。RBN012759 可以降低肿瘤前巨噬细胞的功能并引起肿瘤外植体的炎症反应。

RBN012759

RBN012759 Chemical Structure

CAS No. : 2360851-29-0

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥4400 In-stock
5 mg ¥4000 In-stock
10 mg ¥6800 In-stock
25 mg ¥13500 In-stock
50 mg 询价
100 mg 询价

* Please select Quantity before adding items.

RBN012759 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Epigenetics Compound Library
  • Immunology/Inflammation Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Orally Active Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Targeted Diversity Library

生物活性

RBN012759 is a potent, selective and orally active inhibitor of PARP14, with an IC50 of <3 nm. rbn012759 displays 300-fold selectivity over the monoparps and 1000-fold polyparps. decreases pro-tumor macrophage function elicits inflammatory responses in tumor explants[1].

IC50 & Target[1]

PARP14

<3 nM (IC50)

PARP4

10 μM (IC50)

PARP5a

8 μM (IC50)

PARP5b

10 μM (IC50)

PARP6

4 μM (IC50)

PARP7

4 μM (IC50)

PARP8

20 μM (IC50)

PARP10

1 μM (IC50)

PARP11

1 μM (IC50)

PARP12

5 μM (IC50)

PARP15

3 μM (IC50)

PARP16

6 μM (IC50)

体外研究
(In Vitro)

RBN012759 (0.01-10 μM) decreases the MAR/PAR signal corresponding to PARP14 self MARylation and stabilizes PARP14 protein in a dose-dependent manner in human primary macrophages[1].
RBN012759 (0.1-10 μM) reduces IL-4 stimulated cytokine secretion in human primary macrophages[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

RBN012759 (500 mg/kg BID; p.o.) is well-tolerated in mice with repeat dosing[1].
RBN012759 (100 mg/kg; p.o.) exhibits moderate orally bioavailability (30%) and short plasma half-life (0.4 h) due to moderate clearance (54 mL/min/kg) and low steady-state volume of distribution (1.4 L/kg) in mice[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

378.46

Formula

C19H23FN2O3S

CAS 号

2360851-29-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : 250 mg/mL (660.57 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6423 mL 13.2114 mL 26.4229 mL
5 mM 0.5285 mL 2.6423 mL 5.2846 mL
10 mM 0.2642 mL 1.3211 mL 2.6423 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 (protect from light)。-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% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.50 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.50 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
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.50 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.50 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。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Schenkel L, et, al. A potent and selective PARP14 inhibitor decreases pro-tumor macrophage function and elicits inflammatory responses in tumor explants. AACR Annual Meeting 2020.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务