IACS-13909

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。

IACS-13909  纯度: 99.93%

IACS-13909 是一种有效的选择性的,具有口服活性的 SHP2 变构抑制剂,其 IC50 为 15.7 nM,Kd 为 32 nM。与其他磷酸酶 (包括 SHP1) 相比,IACS-13909 对 SHP2 的选择性更高。IACS-13909 抑制受体酪氨酸激酶 (RTK)/MAPK 途径的信号传导,并具有抗癌作用。

IACS-13909

IACS-13909 Chemical Structure

CAS No. : 2160546-07-4

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3300 In-stock
5 mg ¥3000 In-stock
10 mg ¥5000 In-stock
25 mg ¥10500 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

IACS-13909 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Orally Active Compound Library
  • Phosphatase Inhibitor Library

生物活性

IACS-13909 is a selective, potent and orally active SHP2 allosteric inhibitor with an IC50 of 15.7 nM and a Kd of 32 nM. IACS-13909 is more selective for SHP2 than other phosphatases (including SHP1). IACS-13909 has antitumor activities and suppresses MAPK pathway signaling in receptor tyrosine kinases (RTK)-dependent cancers[1].

IC50 & Target

IC50: 15.7 nM (SHP2)[1]
Kd: 32 nM (SHP2)[1]

体外研究
(In Vitro)

IACS-13909 (10 nM-10 μM; 14 days) treatment potently suppresses the proliferation of wild-type SHP2 and KYSE-520 cells[1].
IACS-13909 (1-5 μM; 2 hours) treatment potently suppresses pERK and pMEK levels in wild-type SHP2 and KYSE-520 cells[1].
IACS-13909 potently suppresses the proliferation of both the parental cells and NCI-H1975 CS cells in a dose-dependent manner, with similar potency (GI50 ~1 μM). IACS-13909 (0.041-3.3 μM) suppresses pERK in NCI-H1975 CS cells in a dose-dependent manner[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.

Cell Proliferation Assay[1]

Cell Line: Wild-type SHP2 and KYSE-520 cells
Concentration: 10 nM, 100 nM, 1 μM, 10 μM
Incubation Time: 14 days
Result: Potently suppressed the cell proliferation.

Western Blot Analysis[1]

Cell Line: Wild-type SHP2 and KYSE-520 cells
Concentration: 1 μM, 5 μM
Incubation Time: 2 hours
Result: Potently suppressed pERK and pMEK levels.

体内研究
(In Vivo)

IACS-13909 (70 mg/kg; oral administration; daily; for 21 days) treatment potently suppresses tumor growth in mice, with 100% tumor growth inhibition (TGI) observed following 21 days of dosing[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.

Animal Model: NSG mice (20-28 g) injected with KYSE-520 cells[1]
Dosage: 70 mg/kg
Administration: Oral administration; daily; for 21 days
Result: Potently suppressed tumor growth in mice.

分子量

377.27

Formula

C17H18Cl2N6

CAS 号

2160546-07-4

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 : 10 mg/mL (26.51 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6506 mL 13.2531 mL 26.5062 mL
5 mM 0.5301 mL 2.6506 mL 5.3012 mL
10 mM 0.2651 mL 1.3253 mL 2.6506 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: ≥ 1 mg/mL (2.65 mM); Clear solution

    此方案可获得 ≥ 1 mg/mL (2.65 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 10.0 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

*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]. Yuting Sun, et al. Allosteric SHP2 Inhibitor, IACS-13909, Overcomes EGFR-Dependent and EGFR-Independent Resistance Mechanisms toward Osimertinib. Cancer Res. 2020 Nov 1;80(21):4840-4853.

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IACS-9571(Synonyms: ASIS-P040)

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。

IACS-9571 (Synonyms: ASIS-P040)

IACS-9571 是溴结构域蛋白 TRIM24BRPF1 的抑制剂,对 TRIM24 的 IC50Kd 值分别为 8 nM 和 31 nM,对 BRPF1 的 Kd 值为 14 nM。

IACS-9571(Synonyms: ASIS-P040)

IACS-9571 Chemical Structure

CAS No. : 1800477-30-8

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

IACS-9571 的其他形式现货产品:

IACS-9571 hydrochloride

生物活性

IACS-9571 is a potent and selective inhibitor of TRIM24 and BRPF1, with IC50 of 8 nM for TRIM24, and Kds of 31 nM and 14 nM for TRIM24 and BRPF1, respectively.

IC50 & Target

IC50: 8 nM (TRIM24)[1]
Kd: 31 nM (TRIM24), 14 nM (BRPF1)[1]

体外研究
(In Vitro)

IACS-9571 shows excellent cellular potency with EC50 of 50 nM. IACS-9571 (1 μM) has potent activities against a panel of 32 bromodomains. IACS-9571 is a selective dual TRIM24/BRPF1 inhibitor (Kd = 1.3/2.1 nM) with 9- and 21-fold selectivity against BRPF2 and BRPF3, respectively. IACS-9571 does not interact with the BET sub-family of bromodomains, displaying greater than 7,700-fold selectivity versus BRD4(1, 2) relative to TRIM24[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

642.76

Formula

C32H42N4O8S

CAS 号

1800477-30-8

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]. Palmer WS, et al. Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor. J Med Chem. 2016 Feb 25;59(4):1440-54.

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IACS-8803

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。

IACS-8803 

IACS-8803 是一种高效环状二核苷酸的 STING 激动剂,具有较强的全身抗肿瘤作用。

IACS-8803

IACS-8803 Chemical Structure

CAS No. : 2095690-70-1

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

IACS-8803 的其他形式现货产品:

IACS-8803 disodium IACS-8803 diammonium

生物活性

IACS-8803 is a highly potent cyclic dinucleotide STING agonist with robust systemic antitumor efficacy[1].

IC50 & Target

STING[1]

体内研究
(In Vivo)

IACS-8803 shows a superior systemic anti-tumor response in the B16 murine model of melanoma[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

692.53

Formula

C20H23FN10O9P2S2

CAS 号

2095690-70-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

H2O : 15 mg/mL (21.66 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.4440 mL 7.2199 mL 14.4398 mL
5 mM 0.2888 mL 1.4440 mL 2.8880 mL
10 mM 0.1444 mL 0.7220 mL 1.4440 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 (sealed storage, away from moisture)。-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。

参考文献
  • [1]. Ager CR, et al. Discovery of IACS-8803 and IACS-8779, potent agonists of stimulator of interferon genes (STING) with robust systemic antitumor efficacy. Bioorg Med Chem Lett. 2019 Oct 15;29(20):126640.

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IACS-9571 hydrochloride(Synonyms: ASIS-P040 hydrochloride)

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。

IACS-9571 hydrochloride (Synonyms: ASIS-P040 hydrochloride) 纯度: 99.28%

IACS-9571 (ASIS-P040) hydrochloride 是溴结构域蛋白 TRIM24BRPF1 的抑制剂,对 TRIM24 的 IC50Kd 值分别为 8 nM 和 31 nM,对 BRPF1 的 Kd 值为 14 nM。

IACS-9571 hydrochloride(Synonyms: ASIS-P040 hydrochloride)

IACS-9571 hydrochloride Chemical Structure

CAS No. : 2319611-93-1

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥5230 In-stock
1 mg ¥1200 In-stock
5 mg ¥3500 In-stock
10 mg ¥6500 In-stock
50 mg ¥22500 In-stock
100 mg ¥33000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

IACS-9571 hydrochloride 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Epigenetics Compound Library
  • Histone Modification Research Compound Library
  • Anti-Cancer Compound Library
  • Reprogramming Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

IACS-9571 (ASIS-P040) hydrochloride is a potent and selective inhibitor of TRIM24 and BRPF1, with an IC50 of 8 nM for TRIM24, and Kds of 31 nM and 14 nM for TRIM24 and BRPF1, respectively[1].

IC50 & Target

IC50: 8 nM (TRIM24)[1]
Kd: 31 nM (TRIM24), 14 nM (BRPF1)[1]

体外研究
(In Vitro)

IACS-9571 Hydrochloride shows excellent cellular potency with EC50 of 50 nM. IACS-9571 Hydrochloride (1 μM) has potent activities against a panel of 32 bromodomains. IACS-9571 Hydrochloride is a selective dual TRIM24/BRPF1 inhibitor (Kd=1.3/2.1 nM) with 9- and 21-fold selectivity against BRPF2 and BRPF3, respectively. IACS-9571 Hydrochloride does not interact with the BET sub-family of bromodomains, displaying greater than 7700-fold selectivity versus BRD4 (1, 2) relative to TRIM24[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

679.22

Formula

C32H43ClN4O8S

CAS 号

2319611-93-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 125 mg/mL (184.03 mM; Need ultrasonic and warming)

H2O : 10 mg/mL (14.72 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.4723 mL 7.3614 mL 14.7228 mL
5 mM 0.2945 mL 1.4723 mL 2.9446 mL
10 mM 0.1472 mL 0.7361 mL 1.4723 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 (sealed storage, away from moisture)。-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。

参考文献
  • [1]. Palmer WS, et al. Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor. J Med Chem. 2016 Feb 25;59(4):1440-54.

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

IACS-010759(Synonyms: IACS-10759)

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。

IACS-010759 (Synonyms: IACS-10759) 纯度: 99.60%

IACS-010759 是一种口服有效的线粒体氧化磷酸化复合物 I (OXPHOS) 抑制剂。IACS-010759 在依赖 OXPHOS 的脑癌和急性髓性白血病 (AML) 模型中抑制增殖并诱导细胞凋亡。IACS-010759 具有用于复发/难治性 AML 和实体瘤研究的潜力。

IACS-010759(Synonyms: IACS-10759)

IACS-010759 Chemical Structure

CAS No. : 1570496-34-2

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1485 In-stock
5 mg ¥1200 In-stock
10 mg ¥2000 In-stock
25 mg ¥4000 In-stock
50 mg ¥6500 In-stock
100 mg ¥9000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

IACS-010759 相关产品

相关化合物库:

  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Metabolism/Protease Compound Library
  • Stem Cell Signaling Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Anti-Aging Compound Library
  • Reprogramming Compound Library
  • Orally Active Compound Library
  • Glutamine Metabolism Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Anti-Parkinson’s Disease Compound Library
  • Neurodegenerative Disease-related Compound Library
  • Mitochondria-Targeted Compound Library
  • Glucose Metabolism Compound Library

生物活性

IACS-010759 is an orally active, potent mitochondrial complex I of oxidative phosphorylation (OXPHOS) inhibitor. IACS-010759 inhibits proliferation and induces apoptosis in models of brain cancer and acute myeloid leukemia (AML) reliant on OXPHOS. IACS-010759 has the potential for relapsed/refractory AML and solid tumors research[1][2].

IC50 & Target

OXPHOS[1]

体外研究
(In Vitro)

IACS-010759 (10, 30, 100 nM; for 4 or 5 days) reduces viability and induces apoptosis in primary AML[1].
IACS-010759 (0.001, 0.01, 0.1, 1, 10, 100, 1000 nM; 72 hurs) robustly inhibits both OCR and galactose-dependent H460 cell viability and has nearly identical IC50 values of 1.4 nM[1].
IACS-010759 is similarly active in mouse (average IC50 = 5.6 nM), rat (IC50 = 12.2 nM), and cynomolgus monkey (IC50 = 8.7 nM) cell lines[1].
IACS-010759 (0.01-10 μM) yieldes a maximal reduction of growth of > 50% in the majority of cancer cell lines (24 of 30 pancreatic (PDAC), 19 of 20 ovarian, 13 of 16 triple-negative breast (TNBC), 8 of 10 non-small-cell lung (NSCLC)) and a subset (11of 30 PDAC, 10 of 20 ovarian, 5 of 16 TNBC, 2 of 10 NSCLC) exhibited > 100% growth inhibition[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)

IACS-010759 (5, 10, 25 mg/kg/day; oral; for 21 d) results in tumor regression with minimal body weight loss at the 5 or 10 mg/kg dose in mice bearing NB-1 (PGD-null) subcutaneous xenografts. IACS-010759 at the 25 mg/kg dose is not tolerated[1].
IACS-010759 HCl (10 mg/kg; orally; QD (daily) or QD×5 (5 d on/2 d off); for 35 d) increases median survival from 28 d to longer than 60 d, whereas less-frequent dosing schedules (Q2D or Q3D) enhances survival to a lesser extent[1].
IACS-010759 (0.3 mg/kg for iv; 1 mg/kg for oral) has low plasma clearance with a high volume of distribution, resulting in a prolonged terminal half-life (>24 h)[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.

Clinical Trial

分子量

562.56

Formula

C25H25F3N6O4S

CAS 号

1570496-34-2

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 : 62.5 mg/mL (111.10 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7776 mL 8.8879 mL 17.7759 mL
5 mM 0.3555 mL 1.7776 mL 3.5552 mL
10 mM 0.1778 mL 0.8888 mL 1.7776 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 (3.70 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (3.70 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    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% corn oil

    Solubility: ≥ 2.08 mg/mL (3.70 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.70 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]. Jennifer R Molina, et al. An inhibitor of oxidative phosphorylation exploits cancer vulnerability. Nat Med. 2018 Jul;24(7):1036-1046.

    [2]. Protopopova M. IACS-10759: A novel OXPHOS inhibitor which selectively kill tumors with metabolic vulnerabilities. [abstract]. In: Proceedings of the 106th Annual Meeting of the American Association for Cancer Research; 2015 Apr 18-22; Philadelphia, PA. Philadelphia (PA): AACR; Cancer Res 2015;75(15 Suppl):Abstract nr 4380. doi:10.1158/1538-7445.AM2015-4380

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

IACS-8803 disodium

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。

IACS-8803 disodium  纯度: 99.15%

IACS-8803 disodium 是一种高效环状二核苷酸的 STING 激动剂,具有强大的全身抗肿瘤作用。

IACS-8803 disodium

IACS-8803 disodium Chemical Structure

CAS No. : 2243079-36-7

规格 价格 是否有货 数量
1 mg ¥5500 In-stock
5 mg ¥14500 In-stock
10 mg   询价  
50 mg   询价  

* Please select Quantity before adding items.

IACS-8803 disodium 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Macrocyclic Compound Library

生物活性

IACS-8803 disodium is a highly potent cyclic dinucleotide STING agonist. IACS-8803 disodium has a robust systemic antitumor efficacy[1].

体内研究
(In Vivo)

IACS-8803 (10 µg; intra-tumoral injection) shows superior antitumor activity in mice bearing bilateral B16-OVA melanomas[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

738.51

Formula

C20H23FN10Na2O9P2S2

CAS 号

2243079-36-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据
In Vitro: 

H2O : 56.67 mg/mL (76.74 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.3541 mL 6.7704 mL 13.5408 mL
5 mM 0.2708 mL 1.3541 mL 2.7082 mL
10 mM 0.1354 mL 0.6770 mL 1.3541 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 (stored under nitrogen)。-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。

参考文献
  • [1]. Ager CR, et al. Discovery of IACS-8803 and IACS-8779, potent agonists of stimulator of interferon genes (STING) with robust systemic antitumor efficacy. Bioorg Med Chem Lett. 2019 Oct 15;29(20):126640.

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IACS-8779

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。

IACS-8779 

IACS-8779 是干扰素基因刺激剂 (STING) 的强效激动剂,具有强大的全身性抗肿瘤功效。

IACS-8779

IACS-8779 Chemical Structure

CAS No. : 2243079-26-5

规格 是否有货
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生物活性

IACS-8779 is a highly potent stimulator of interferon genes (STING) agonist with robust systemic antitumor efficacy[1].

体内研究
(In Vivo)

Mice are implanted bilaterally with B16-Ova, and IACS-8779 (compound 1a) is administered at 10 μg dose with three intra-tumoral injections, on one flank only, on day 6, 9, 12 post implantation. While IACS-8779 shows comparable antitumor activity on the injected flank, IACS-8779 achieves superior regression on the untreated tumor in the contralateral flank, suggesting a more significant systemic immune response compared to the benchmark analogs. Treatment with IACS-8779 also results in a higher number of mice cured of both tumors compared to benchmarks[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

689.56

Formula

C21H25N9O10P2S2

CAS 号

2243079-26-5

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]. Ager CR, et al. Discovery of IACS-8803 and IACS-8779, potent agonists of stimulator of interferon genes (STING) with robust systemic antitumor efficacy. Bioorg Med Chem Lett. 2019 Oct 15;29(20):126640.

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IACS-8803 diammonium

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。

IACS-8803 diammonium  纯度: 99.24%

IACS-8803 diammonium 是一种高效环状二核苷酸的 STING 激动剂,具有强大的全身抗肿瘤作用。

IACS-8803 diammonium

IACS-8803 diammonium Chemical Structure

规格 价格 是否有货 数量
1 mg ¥5500 In-stock
5 mg ¥14500 In-stock
10 mg   询价  
50 mg   询价  

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IACS-8803 diammonium 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Macrocyclic Compound Library

生物活性

IACS-8803 diammonium is a highly potent cyclic dinucleotide STING agonist. IACS-8803 diammonium has a robust systemic antitumor efficacy[1].

体内研究
(In Vivo)

IACS-8803 diammonium (10 µg; intra-tumoral injection) shows superior antitumor activity in mice bearing bilateral B16-OVA melanomas[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

726.60

Formula

C20H29FN12O9P2S2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献
  • [1]. Ager CR, et al. Discovery of IACS-8803 and IACS-8779, potent agonists of stimulator of interferon genes (STING) with robust systemic antitumor efficacy. Bioorg Med Chem Lett. 2019 Oct 15;29(20):126640.

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IACS-15414

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。

IACS-15414 

IACS-15414 是一种口服有效的 SHP2 抑制剂,IC50 值为 122 nM。

IACS-15414

IACS-15414 Chemical Structure

CAS No. : 2411321-29-2

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

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生物活性

IACS-15414 is a potent and orally bioavailable SHP2 inhibitor with an IC50 value of 122 nM.

分子量

423.34

Formula

C20H24Cl2N4O2

CAS 号

2411321-29-2

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]. Czako B, et al. Discovery of 6-[(3S,4S)-4-Amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-3-(2,3-dichlorophenyl)-2-methyl-3,4-dihydropyrimidin-4-one (IACS-15414), a Potent and Orally Bioavailable SHP2 Inhibitor. J Med Chem. 2021 Oct 28;64(20):15141-15169.

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IACS-010759 hydrochloride(Synonyms: IACS-10759 hydrochloride)

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。

IACS-010759 hydrochloride (Synonyms: IACS-10759 hydrochloride) 纯度: 99.58%

IACS-010759 是一种口服有效的线粒体氧化磷酸化复合物 I (OXPHOS) 抑制剂。IACS-010759 在依赖 OXPHOS 的脑癌和急性髓性白血病 (AML) 模型中抑制增殖并诱导细胞凋亡。IACS-010759 具有用于复发/难治性 AML 和实体瘤研究的潜力。

IACS-010759 hydrochloride(Synonyms: IACS-10759 hydrochloride)

IACS-010759 hydrochloride Chemical Structure

CAS No. : 1807523-99-4

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1581 In-stock
5 mg ¥1200 In-stock
10 mg ¥2000 In-stock
25 mg ¥4000 In-stock
50 mg ¥6500 In-stock
100 mg ¥9000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

IACS-010759 hydrochloride 相关产品

相关化合物库:

  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Metabolism/Protease Compound Library
  • Stem Cell Signaling Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Anti-Aging Compound Library
  • Reprogramming Compound Library
  • Orally Active Compound Library
  • Glutamine Metabolism Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Anti-Parkinson’s Disease Compound Library
  • Neurodegenerative Disease-related Compound Library
  • Mitochondria-Targeted Compound Library
  • Glucose Metabolism Compound Library

生物活性

IACS-010759 hydrochlorideis an orally active, potent mitochondrial complex I of oxidative phosphorylation (OXPHOS) inhibitor. IACS-010759 hydrochlorideinhibits proliferation and induces apoptosis in models of brain cancer and acute myeloid leukemia (AML) reliant on OXPHOS. IACS-010759 hydrochloride has the potential for relapsed/refractory AML and solid tumors research[1][2].

IC50 & Target

OXPHOS[1]

体外研究
(In Vitro)

IACS-010759 hydrochloride (10, 30, 100 nM; for 4 or 5 days) reduces viability and induces apoptosis in primary AML[1].
IACS-010759 hydrochloride (0.001, 0.01, 0.1, 1, 10, 100, 1000 nM; 72 hurs) robustly inhibits both OCR and galactose-dependent H460 cell viability and has nearly identical IC50 values of 1.4 nM[1].
IACS-010759 hydrochlorideis similarly active in mouse (average IC50 = 5.6 nM), rat (IC50 = 12.2 nM), and cynomolgus monkey (IC50 = 8.7 nM) cell lines[1].
IACS-010759 hydrochloride (0.01-10 μM) yieldes a maximal reduction of growth of > 50% in the majority of cancer cell lines (24 of 30 pancreatic (PDAC), 19 of 20 ovarian, 13 of 16 triple-negative breast (TNBC), 8 of 10 non-small-cell lung (NSCLC)) and a subset (11of 30 PDAC, 10 of 20 ovarian, 5 of 16 TNBC, 2 of 10 NSCLC) exhibited > 100% growth inhibition[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)

IACS-010759 hydrochloride (5, 10, 25 mg/kg/day; oral; for 21 d) results in tumor regression with minimal body weight loss at the 5 or 10 mg/kg dose in mice bearing NB-1 (PGD-null) subcutaneous xenografts. IACS-010759 at the 25 mg/kg dose is not tolerated[1].
IACS-010759 HCl (10 mg/kg; orally; QD (daily) or QD×5 (5 d on/2 d off); for 35 d) increases median survival from 28 d to longer than 60 d, whereas less-frequent dosing schedules (Q2D or Q3D) enhances survival to a lesser extent[1].
IACS-010759 hydrochloride (0.3 mg/kg for iv; 1 mg/kg for oral) has low plasma clearance with a high volume of distribution, resulting in a prolonged terminal half-life (>24 h)[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.

Clinical Trial

分子量

599.02

Formula

C25H26ClF3N6O4S

CAS 号

1807523-99-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 60 mg/mL (100.16 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.6694 mL 8.3470 mL 16.6939 mL
5 mM 0.3339 mL 1.6694 mL 3.3388 mL
10 mM 0.1669 mL 0.8347 mL 1.6694 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 (sealed storage, away from moisture)。-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% corn oil

    Solubility: ≥ 2.5 mg/mL (4.17 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.17 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 25.0 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]. Protopopova M. IACS-10759: A novel OXPHOS inhibitor which selectively kill tumors with metabolic vulnerabilities. [abstract]. In: Proceedings of the 106th Annual Meeting of the American Association for Cancer Research; 2015 Apr 18-22; Philadelphia, PA. Philadelphia (PA): AACR; Cancer Res 2015;75(15 Suppl):Abstract nr 4380. doi:10.1158/1538-7445.AM2015-4380

    [2]. Jennifer R Molina, et al. An inhibitor of oxidative phosphorylation exploits cancer vulnerability. Nat Med. 2018 Jul;24(7):1036-1046.

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IACS-8779 disodium

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。

IACS-8779 disodium 

IACS-8779 disodium 是一种高效的干扰素基因刺激蛋白 (STING) 激动剂,具有强大的全身性抗肿瘤功效。IACS-8779 disodium 在 B16 小鼠黑色素瘤模型中对 STING 通路具有强烈活性,且具有卓越的抗肿瘤作用。

IACS-8779 disodium

IACS-8779 disodium Chemical Structure

CAS No. : 2243079-27-6

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

IACS-8779 disodium is a highly potent stimulator of interferon genes (STING) agonist with robust systemic antitumor efficacy. IACS-8779 disodium shows robust activation of the STING pathway in vitro and a superior systemic anti-tumor response in the B16 murine model of melanoma[1].

分子量

733.52

Formula

C21H23N9Na2O10P2S2

CAS 号

2243079-27-6

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]. Ager CR, et al. Discovery of IACS-8803 and IACS-8779, potent agonists of stimulator of interferon genes (STING) with robust systemic antitumor efficacy. Bioorg Med Chem Lett. 2019 Oct 15;29(20):126640.

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