Mutant p53 modulator-1

发表于2024年4月14日由上海金畔生物科技有限公司

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。

Mutant p53 modulator-1

Mutant p53 modulator-1 是一种突变型 p53 调节剂。Mutant p53 modulator-1 可减少含有 p53 突变的癌症的进展 (摘自专利 WO2021231474A1，化合物 231B)。

Mutant p53 modulator-1 Chemical Structure

CAS No. : 2746371-35-5

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生物活性	Mutant p53 modulator-1 is a mutant p53 modulator. Mutant p53 modulator-1 reduces the progression of cancers that contain a p53 mutation (extracted from patent WO2021231474A1, compound 231B)^[1].
分子量	576.59
Formula	C₂₇H₃₂F₄N₈O₂
CAS 号	2746371-35-5
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]. Binh Vu, et al. METHODS AND COMPOUNDS FOR RESTORING MUTANT p53 FUNCTION. Patent WO2021231474A1.

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Estrogen receptor modulator 1

发表于2024年3月9日由上海金畔生物科技有限公司

Estrogen receptor modulator 1

Estrogen receptor modulator 1 (compound 18) 是一种口服活性选择性雌激素受体 (estrogen receptor) 调节剂 (SERM)，pIC₅₀ 为 0.46。Estrogen receptor modulator 1 诱导 Tamoxifen 耐药、激素非依赖性异种移植瘤的消退。

Estrogen receptor modulator 1 Chemical Structure

CAS No. : 63676-22-2

规格	价格	是否有货
10 mg	￥1400	询问价格 & 货期

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生物活性

Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM), with a pIC₅₀ of 0.46. Estrogen receptor modulator 1 induces regression of Tamoxifen-resistant, hormone independent xenograft tumors^[1]^[2].

体外研究
(In Vitro)

Estrogen receptor modulator 1 (compound 18) (100 nM; 10 days) inhibits T47D:A18/PKCα and T47D:A18-TAM1 colony formation^[2].
Estrogen receptor modulator 1 (100 nM; 9 days) significantly inhibits the growth of MCF-7:5C cell, and induces apoptosis in these cells 6 days^[2].

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

Cell Proliferation Assay^[2]

Cell Line:	T47D:A18/PKCα and T47D:A18-TAM1 cells
Concentration:	100 nM
Incubation Time:	10 days
Result:	Inhibit T47D:A18/PKCα and T47D:A18-TAM1 colony formation.

Cell Viability Assay^[2]

Cell Line:	MCF-7:5C cells
Concentration:	100 nM
Incubation Time:	9 days
Result:	Significantly inhibited the growth of MCF-7:5C cells.

体内研究
(In Vivo)

Estrogen receptor modulator 1 (1.5 mg/animal; p.o. ; daily for 2 weeks) results in regression of T47D:A18/PKCα tumors^[2].

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

Animal Model:	4-6 week old athymic mice (Harlan-Sprague-Dawley)^[2]
Dosage:	1.5 mg/animal
Administration:	p.o. ; daily for 2 weeks
Result:	Significantly reduced tumor volume.

分子量

242.29

Formula

C₁₄H₁₀O₂S

CAS 号

63676-22-2

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]. Brogi S, et al. 3D-QSAR using pharmacophore-based alignment and virtual screening for discovery of novel MCF-7 cell line inhibitors. Eur J Med Chem. 2013 Sep;67:344-51.

[2]. Molloy ME, et al. Novel selective estrogen mimics for the treatment of tamoxifen-resistant breast cancer. Mol Cancer Ther. 2014 Nov;13(11):2515-26.

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Sirtuin modulator 1

发表于2024年3月9日由上海金畔生物科技有限公司

Sirtuin modulator 1 纯度: 99.72%

Sirtuin modulator 1 是 SIRTl (SIRT3 的同系物) 的调节剂，EC_1.5 值 < 1 μM，摘自专利 WO 2010071853 A1，化合物 4。

Sirtuin modulator 1 Chemical Structure

CAS No. : 2070015-26-6

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1730	In-stock
1 mg	￥650	In-stock
5 mg	￥1300	In-stock
10 mg	￥2250	In-stock
50 mg	￥6750	In-stock
100 mg	￥11500	In-stock
200 mg		询价
500 mg		询价

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Sirtuin modulator 1 相关产品

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Cell Cycle/DNA Damage Compound Library
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Anti-Cancer Compound Library
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Diabetes Related Compound Library
Oxygen Sensing Compound Library
Glutamine Metabolism Compound Library

生物活性

Sirtuin modulator 1 is a modulator of SIRTl, a homolog of SIRT3, with EC_1.5 of < 1 μM, extracted from patent WO 2010071853 A1, Compound No.4.

IC₅₀ & Target^[1]

SIRT1

1 μM (EC1.5)

分子量

606.20

Formula

C₃₁H₃₂ClN₅O₂S₂

CAS 号

2070015-26-6

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 : 12.5 mg/mL (20.62 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6496 mL	8.2481 mL	16.4962 mL
5 mM	0.3299 mL	1.6496 mL	3.2992 mL
10 mM	0.1650 mL	0.8248 mL	1.6496 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 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 1.25 mg/mL (2.06 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (2.06 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 12.5 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: ≥ 1.25 mg/mL (2.06 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (2.06 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 12.5 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

*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]. Thiazolopyridine sirtuin modulating compounds. WO 2010071853 A1

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AhR modulator-1

发表于2024年3月7日由上海金畔生物科技有限公司

AhR modulator-1

AhR modulator-1 (compound 6-MCDF) 是一种选择性的口服活性芳烃受体 (AhR) 调节剂。AhR modulator-1 部分地通过在肿瘤形成之前抑制前列腺 VEGF 的产生而抑制肿瘤转移。AhR modulator-1 在大鼠子宫中也具有抗雌激素特性。

AhR modulator-1 Chemical Structure

CAS No. : 115039-00-4

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生物活性

AhR modulator-1 (compound 6-MCDF) is a selective and orally active aryl hydrocarbon receptor (AhR) modulator. AhR modulator-1 inhibits metastasis, in part, by inhibiting prostatic VEGF production prior to tumor formation. AhR modulator-1 also possess anti-estrogenic properties in rat uterus^[1].

IC₅₀ & Target

Aryl hydrocarbon receptor (AhR) ^[1]^[2]
Prostatic VEGF^[1]
Estrogenic^[1]

体外研究
(In Vitro)

AhR modulator-1 (6-MCDF; 0.1-10 μM; 48-96 hours; ASPC-1 cells) treatment exhibits dose-dependent growth inhibitory effects with growth inhibitory effects of 26, 43 and 99% at concentrations of 0.1, 1 and 10 μM, respectively^[2].

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

Cell Proliferation Assay^[2]

Cell Line:	ASPC-1 cells
Concentration:	0.1 μM, 1 μM and 10 μM
Incubation Time:	48 hours, 72 hours, 96 hours
Result:	Exhibited dose-dependent growth inhibitory effects.

体内研究
(In Vivo)

AhR modulator-1 (6-MCDF; 0-40 mg/kg; oral administration; daily; for 12 weeks; C57BL/6-Tg(TRAMP)8247Ng/J mice) treatment reduces the frequency of pelvic lymph node metastasis in mice fed the 40 mg/kg diet. And serum VEGF concentrations are also reduced. Prostate tumor incidence and size are not significantly reduced^[1].

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

Animal Model:	C57BL/6-Tg(TRAMP)8247Ng/J (TRAMP) mice (8-week-old)^[1]
Dosage:	0 mg/kg, 10 mg/kg, 40 mg/kg
Administration:	Oral administration; daily; for 12 weeks
Result:	The frequency of pelvic lymph node metastasis was reduced 5-fold in mice fed the 40 mg /kg diet.S erum VEGF concentrations were also reduced.

分子量

285.55

Formula

C₁₃H₇Cl₃O

CAS 号

115039-00-4

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]. Fritz WA, et al. The selective aryl hydrocarbon receptor modulator 6-methyl-1,3,8-trichlorodibenzofuran inhibits prostate tumor metastasis in TRAMP mice. Biochem Pharmacol. 2009 Apr 1;77(7):1151-60.

[2]. Koliopanos A, et al. Increased arylhydrocarbon receptor expression offers a potential therapeutic target for pancreatic cancer. Oncogene. 2002 Sep 5;21(39):6059-70.

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Autotaxin modulator 1

发表于2024年2月20日由上海金畔生物科技有限公司

Autotaxin modulator 1 纯度: 98.93%

Autotaxin modulator 1 是一种自分泌运动因子 autotaxin (ATX) 抑制剂，详细信息请参考专利文献 WO 2014018881 A1 中的化合物案例 12b。Autotaxin modulator 1 有望用于损伤或疾病引起的脱髓鞘，以及肿瘤等增生性疾病的研究。

Autotaxin modulator 1 Chemical Structure

CAS No. : 1548743-69-6

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1790	In-stock
5 mg	￥1500	In-stock
10 mg	￥2500	In-stock
50 mg	￥7500	In-stock
100 mg	￥12500	In-stock
200 mg		询价
500 mg		询价

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Autotaxin modulator 1 相关产品

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生物活性

Autotaxin modulator 1 is an autotaxin (ATX) enzyme inhibitor, extracted from patent WO 2014018881 A1, Compound Example 12b. Autotaxin modulator 1 is expected to be useful for researching demyelination due to injury or disease, as well as for researching proliferative disorders such as cancer^[1].

IC₅₀ & Target^[1]

Autotaxin

体外研究
(In Vitro)

Autotaxin, a novel motility-stimulating protein, is a secreted glycoprotein widely present in biological fluids, including blood, cancer ascites, synovial, pleural and cerebrospinal fluids, originally isolated from the supernatant of melanoma cells as an autocrine motility stimulation factor^[1].
Autotaxin is a member of the ectonucleotide pyrophosphatase/phosphodiesterase family of ectoenzymes (E-NPP) that hydrolyze phosphodiesterase (PDE) bonds of various nucleotides and derivatives^[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

543.54

Formula

C₂₈H₃₁F₆NO₃

CAS 号

1548743-69-6

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 (183.98 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8398 mL	9.1990 mL	18.3979 mL
5 mM	0.3680 mL	1.8398 mL	3.6796 mL
10 mM	0.1840 mL	0.9199 mL	1.8398 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：

1.

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

Solubility: ≥ 2.5 mg/mL (4.60 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.60 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 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
2.

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

Solubility: ≥ 2.5 mg/mL (4.60 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.60 mM，饱和度未知) 的澄清溶液。

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 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: ≥ 2.5 mg/mL (4.60 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.60 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]. Guckian, Kevin, et al. Preparation of naphthalenes and isoquinolines as ATX modulating agents. WO 2014018881 A1.

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CRBN modulator-1

发表于2024年2月15日由上海金畔生物科技有限公司

CRBN modulator-1 纯度: 98.06%

CRBN modulator-1，一种 Thalidomide 类似物和 CRBN 调节剂，结合 CRBN 的IC₅₀ 值和 K_i 值分别为 3.5 μM 和 0.98 μM。

CRBN modulator-1 Chemical Structure

CAS No. : 2407829-65-4

规格	价格	是否有货
5 mg	￥1500	In-stock
10 mg	￥2500	In-stock
25 mg	￥4500	In-stock
50 mg	￥7500	In-stock
100 mg	￥12500	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

CRBN modulator-1 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Anti-Cancer Compound Library
Ubiquitination Compound Library

生物活性

CRBN modulator-1, a Thalidomide analog and a CRBN modulator extracted from WO2020006262A1, compound 10, has an IC₅₀ of 3.5 μM and a K_i of 0.98 μM^[1].

IC₅₀ & Target^[1]

Cereblon

分子量

324.29

Formula

C₁₇H₁₂N₂O₅

CAS 号

2407829-65-4

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 (30.84 mM; ultrasonic and adjust pH to 2 with HCl)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.0837 mL	15.4183 mL	30.8366 mL
5 mM	0.6167 mL	3.0837 mL	6.1673 mL
10 mM	0.3084 mL	1.5418 mL	3.0837 mL

参考文献

[1]. Nathanael Gray, et al. New crbn modulators. WO2020006262A1.

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Nur77 modulator 1

发表于2024年1月4日由上海金畔生物科技有限公司

Nur77 modulator 1 纯度: 98.23%

Nur77 modulator 1 可结合到Nur77 (K_D = 3.58 μM)。Nur77 modulator 1 上调 Nur77 表达，介导Nur77亚细胞定位，诱导Nur77 依赖的内质网应激和自噬，可导致细胞凋亡。抗肝癌生物活性。

Nur77 modulator 1 Chemical Structure

CAS No. : 2469975-55-9

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥3820	In-stock
5 mg	￥3500	In-stock
10 mg	￥5800	In-stock
25 mg	￥11000	In-stock
50 mg	￥17000	In-stock
100 mg	￥25000	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

Nur77 modulator 1 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Apoptosis Compound Library
Anti-Cancer Compound Library
Endoplasmic Reticulum Stress Compound Library
Anti-Liver Cancer Compound Library

生物活性

Nur77 modulator 1 is a good Nur77 binder (K_D = 3.58 μM). Nur77 modulator 1 up-regulates Nur77 expression, mediates sub-cellular localization of Nur77, induces Nur77-dependent ER stress and autophagy, and results in cell apoptosis. Anti-hepatoma activity^[1].

IC₅₀ & Target

KD: 3.58 μM (Nur77) ^[1].

体外研究
(In Vitro)

Nur77 modulator 1 (10g, 0-20 μM) displays potent and broad-spectrum antiproliferative activity against all tested three hepatoma cell lines (HepG2, QGY-7703, and SMMC-7721), and less cytotoxicity against LO2 cells (human normal liver cell line)^[1].
Nur77 modulator 1 (10g, ) could specifically up-regulate the expression of Nur77 in a dose-dependent manner^[1].
Nur77 modulator 1 (10g, 2.0 μM) induces Nur77-dependent apoptosis^[1].
Nur77 modulator 1 (10g, 2.0 μM) increased LC3-II and Beclin1 protein levels in a dose-dependent manner (10g treatment does not enhance p62 degradation, indicating that autophagy induced by 10g is incomplete)^[1].

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

Cell Viability Assay^[1].

Cell Line:	Liver cancer cell lines (HepG2, QGY-7703, and SMMC-7721).
Concentration:	0-20 μM.
Incubation Time:	12-24 hours.
Result:	Exhibited IC₅₀ values of 0.6 µM, 0.89 µM, 1.40 µM and >20 µM in HepG2, QGY-7703, SMMC-7721 and LO2 cells, respectively. Reduced the viability in a time-dependent manner. Induced cell morphology alteration, such as cell shrinkage, vesicles accumulated, and reduced cell number.

体内研究
(In Vivo)

Nur77 modulator 1 (10g, 10 and 20 mg/kg/day) exhibits significant anti-tumor activity in mouse hepatoma HepG2 xenograft with good tolerability^[1].

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

Animal Model:	Nude mouse hepatoma HepG2 xenograft^[1].
Dosage:	10 and 20 mg/kg/day.
Administration:	IP, once every day for 15 days.
Result:	Lead to substantial suppression of tumor growth. The tumor growth inhibition (TGI) values at doses of 10mg/kg/day and 20 mg/kg/day were 36.74 % and 62.38 %, respectively. Exhibited almost no influence on the body weight of experimental mice.

分子量

495.60

Formula

C₂₈H₂₅N₅O₂S

CAS 号

2469975-55-9

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 : 125 mg/mL (252.22 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0178 mL	10.0888 mL	20.1776 mL
5 mM	0.4036 mL	2.0178 mL	4.0355 mL
10 mM	0.2018 mL	1.0089 mL	2.0178 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：

1.

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

Solubility: 2.08 mg/mL (4.20 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (4.20 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 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 (4.20 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.20 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 Shanghai Jinpan Biotech Co Ltd 网站选购。

参考文献

[1]. Baicun Li, et al. Design, synthesis, and biological evaluation of 5-((8-methoxy-2-methylquinolin-4-yl)amino)-1H-indole-2-carbohydrazide derivatives as novel Nur77 modulators. Eur J Med Chem. 2020 Oct 15;204:112608.

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

Nur77 modulator 1

发表于2024年1月4日由上海金畔生物科技有限公司

Nur77 modulator 1 纯度: 98.23%

Nur77 modulator 1 Chemical Structure

CAS No. : 2469975-55-9

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥3820	In-stock
5 mg	￥3500	In-stock
10 mg	￥5800	In-stock
25 mg	￥11000	In-stock
50 mg	￥17000	In-stock
100 mg	￥25000	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

Nur77 modulator 1 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Apoptosis Compound Library
Anti-Cancer Compound Library
Endoplasmic Reticulum Stress Compound Library
Anti-Liver Cancer Compound Library

生物活性

IC₅₀ & Target

KD: 3.58 μM (Nur77) ^[1].

体外研究
(In Vitro)

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

Cell Viability Assay^[1].

Cell Line:	Liver cancer cell lines (HepG2, QGY-7703, and SMMC-7721).
Concentration:	0-20 μM.
Incubation Time:	12-24 hours.
Result:	Exhibited IC₅₀ values of 0.6 µM, 0.89 µM, 1.40 µM and >20 µM in HepG2, QGY-7703, SMMC-7721 and LO2 cells, respectively. Reduced the viability in a time-dependent manner. Induced cell morphology alteration, such as cell shrinkage, vesicles accumulated, and reduced cell number.

体内研究
(In Vivo)

Nur77 modulator 1 (10g, 10 and 20 mg/kg/day) exhibits significant anti-tumor activity in mouse hepatoma HepG2 xenograft with good tolerability^[1].

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

Animal Model:	Nude mouse hepatoma HepG2 xenograft^[1].
Dosage:	10 and 20 mg/kg/day.
Administration:	IP, once every day for 15 days.
Result:	Lead to substantial suppression of tumor growth. The tumor growth inhibition (TGI) values at doses of 10mg/kg/day and 20 mg/kg/day were 36.74 % and 62.38 %, respectively. Exhibited almost no influence on the body weight of experimental mice.

分子量

495.60

Formula

C₂₈H₂₅N₅O₂S

CAS 号

2469975-55-9

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 : 125 mg/mL (252.22 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0178 mL	10.0888 mL	20.1776 mL
5 mM	0.4036 mL	2.0178 mL	4.0355 mL
10 mM	0.2018 mL	1.0089 mL	2.0178 mL

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：

1.

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

Solubility: 2.08 mg/mL (4.20 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (4.20 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 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 (4.20 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.20 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 Shanghai Jinpan Biotech Co Ltd 网站选购。

参考文献

[1]. Baicun Li, et al. Design, synthesis, and biological evaluation of 5-((8-methoxy-2-methylquinolin-4-yl)amino)-1H-indole-2-carbohydrazide derivatives as novel Nur77 modulators. Eur J Med Chem. 2020 Oct 15;204:112608.

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

Nur77 modulator 1

发表于2024年1月4日由上海金畔生物科技有限公司

Nur77 modulator 1 纯度: 98.23%

Nur77 modulator 1 Chemical Structure

CAS No. : 2469975-55-9

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥3820	In-stock
5 mg	￥3500	In-stock
10 mg	￥5800	In-stock
25 mg	￥11000	In-stock
50 mg	￥17000	In-stock
100 mg	￥25000	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

Nur77 modulator 1 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Apoptosis Compound Library
Anti-Cancer Compound Library
Endoplasmic Reticulum Stress Compound Library
Anti-Liver Cancer Compound Library

生物活性

IC₅₀ & Target

KD: 3.58 μM (Nur77) ^[1].

体外研究
(In Vitro)

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 Viability Assay^[1].

Cell Line:	Liver cancer cell lines (HepG2, QGY-7703, and SMMC-7721).
Concentration:	0-20 μM.
Incubation Time:	12-24 hours.
Result:	Exhibited IC₅₀ values of 0.6 µM, 0.89 µM, 1.40 µM and >20 µM in HepG2, QGY-7703, SMMC-7721 and LO2 cells, respectively. Reduced the viability in a time-dependent manner. Induced cell morphology alteration, such as cell shrinkage, vesicles accumulated, and reduced cell number.

体内研究
(In Vivo)

Nur77 modulator 1 (10g, 10 and 20 mg/kg/day) exhibits significant anti-tumor activity in mouse hepatoma HepG2 xenograft with good tolerability^[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:	Nude mouse hepatoma HepG2 xenograft^[1].
Dosage:	10 and 20 mg/kg/day.
Administration:	IP, once every day for 15 days.
Result:	Lead to substantial suppression of tumor growth. The tumor growth inhibition (TGI) values at doses of 10mg/kg/day and 20 mg/kg/day were 36.74 % and 62.38 %, respectively. Exhibited almost no influence on the body weight of experimental mice.

分子量

495.60

Formula

C₂₈H₂₅N₅O₂S

CAS 号

2469975-55-9

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 : 125 mg/mL (252.22 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0178 mL	10.0888 mL	20.1776 mL
5 mM	0.4036 mL	2.0178 mL	4.0355 mL
10 mM	0.2018 mL	1.0089 mL	2.0178 mL

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：

1.

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

Solubility: 2.08 mg/mL (4.20 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (4.20 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 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 (4.20 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.20 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]. Baicun Li, et al. Design, synthesis, and biological evaluation of 5-((8-methoxy-2-methylquinolin-4-yl)amino)-1H-indole-2-carbohydrazide derivatives as novel Nur77 modulators. Eur J Med Chem. 2020 Oct 15;204:112608.

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

CXCR4 modulator-1

发表于2023年12月16日由上海金畔生物科技有限公司

CXCR4 modulator-1

CXCR4 modulator-1 (compound ZINC72372983) 是一种有效的 CXCR4 调节剂，EC₅₀ 为 100 nM。CXCR4 modulator-1 可用于研究抗炎、抗癌及抗 HIV 感染。

CXCR4 modulator-1 Chemical Structure

CAS No. : 1381178-26-2

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

CXCR4 modulator-1 (compound ZINC72372983) is a potent CXCR4 modulator with an EC₅₀ value of 100 nM. CXCR4 modulator-1 can be used for researching anti-inflammatory, anticancer and anti-HIV^[1].

IC₅₀ & Target^[1]

CXCR4

100 nM (EC₅₀)

分子量

405.49

Formula

C₂₃H₂₇N₅O₂

CAS 号

1381178-26-2

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]. Oum YH, et al. Discovery of novel aminopiperidinyl amide CXCR4 modulators through virtual screening and rational drug design. Eur J Med Chem. 2020;201:112479.

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

IL-17A modulator-2

发表于2023年12月12日由上海金畔生物科技有限公司

IL-17A modulator-2

IL-17A modulator-2 是一种 IL-17A 调节剂，来自专利 WO2021239743+A1，example 27。IL-17A modulator-2 抑制 IL-17A 的生物学效应，pIC₅₀ 为 8.3。IL-17A modulator-2 可用于研究与调节 IL-17A 活性相关的疾病或病症，包括具有免疫成分或自身免疫病理的疾病、癌症和神经退行性疾病。

IL-17A modulator-2 Chemical Structure

CAS No. : 2748749-47-3

规格	价格	是否有货
5 mg	￥6500	询问价格 & 货期
10 mg	￥10500	询问价格 & 货期

* Please select Quantity before adding items.

生物活性

IL-17A modulator-2 is a IL-17A modulator, extracted from patent WO2021239743+A1, example 27. IL-17A modulator-2 inhibits the biological action of IL-17A with a pIC₅₀ of 8.3. IL-17A modulator-2 can be used for the research of diseases or disorders associated with modulation of IL-17A activity including diseases with an immune component or autoimmune pathol, cancer and neurodegenerative disorders^[1].

IC₅₀ & Target^[1]

IL-17A

8.3 (pIC₅₀)

分子量

577.63

Formula

C₃₃H₃₁N₅O₅

CAS 号

2748749-47-3

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]. Barrie Phillip MARTIN, et al. Preparation of amino acid amides as IL-17A modulators. WO2021239743 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

IL-17A modulator-1

发表于2023年12月12日由上海金畔生物科技有限公司

IL-17A modulator-1

IL-17A modulator-1 是一种 IL-17A 调节剂，来自专利 WO2021239743+A1，example 9。IL-17A modulator-1 抑制 IL-17A 的生物学效应，pIC₅₀ 为 8.2。IL-17A modulator-1 可用于研究与调节 IL-17A 活性相关的疾病或病症，包括具有免疫成分或自身免疫病理的疾病、癌症和神经退行性疾病。

IL-17A modulator-1 Chemical Structure

CAS No. : 2748749-29-1

规格	价格	是否有货
5 mg	￥5800	询问价格 & 货期
10 mg	￥9200	询问价格 & 货期
25 mg	￥18500	询问价格 & 货期

* Please select Quantity before adding items.

生物活性

IL-17A modulator-1 is a IL-17A modulator, extracted from patent WO2021239743+A1, example 9. IL-17A modulator-1 inhibits the biological action of IL-17A with a pIC₅₀ of 8.2. IL-17A modulator-1 can be used for the research of diseases or disorders associated with modulation of IL-17A activity including diseases with an immune component or autoimmune pathol, cancer and neurodegenerative disorders^[1].

IC₅₀ & Target^[1]

IL-17A

8.2 (pIC₅₀)

分子量

561.63

Formula

C₃₃H₃₁N₅O₄

CAS 号

2748749-29-1

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]. Barrie Phillip MARTIN, et al. Preparation of amino acid amides as IL-17A modulators. WO2021239743 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

IL-17A modulator-2

发表于2023年12月12日由上海金畔生物科技有限公司

IL-17A modulator-2

IL-17A modulator-2 Chemical Structure

CAS No. : 2748749-47-3

规格	价格	是否有货
5 mg	￥6500	询问价格 & 货期
10 mg	￥10500	询问价格 & 货期

* Please select Quantity before adding items.

生物活性

IC₅₀ & Target^[1]

IL-17A

8.3 (pIC₅₀)

分子量

577.63

Formula

C₃₃H₃₁N₅O₅

CAS 号

2748749-47-3

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]. Barrie Phillip MARTIN, et al. Preparation of amino acid amides as IL-17A modulators. WO2021239743 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

IL-17A modulator-1

发表于2023年12月12日由上海金畔生物科技有限公司

IL-17A modulator-1

IL-17A modulator-1 Chemical Structure

CAS No. : 2748749-29-1

规格	价格	是否有货
5 mg	￥5800	询问价格 & 货期
10 mg	￥9200	询问价格 & 货期
25 mg	￥18500	询问价格 & 货期

* Please select Quantity before adding items.

生物活性

IC₅₀ & Target^[1]

IL-17A

8.2 (pIC₅₀)

分子量

561.63

Formula

C₃₃H₃₁N₅O₄

CAS 号

2748749-29-1

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]. Barrie Phillip MARTIN, et al. Preparation of amino acid amides as IL-17A modulators. WO2021239743 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

IL-17A modulator-2

发表于2023年12月12日由上海金畔生物科技有限公司

IL-17A modulator-2

IL-17A modulator-2 Chemical Structure

CAS No. : 2748749-47-3

规格	价格	是否有货
5 mg	￥6500	询问价格 & 货期
10 mg	￥10500	询问价格 & 货期

* Please select Quantity before adding items.

生物活性

IC₅₀ & Target^[1]

IL-17A

8.3 (pIC₅₀)

分子量

577.63

Formula

C₃₃H₃₁N₅O₅

CAS 号

2748749-47-3

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]. Barrie Phillip MARTIN, et al. Preparation of amino acid amides as IL-17A modulators. WO2021239743 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

IL-17A modulator-1

发表于2023年12月12日由上海金畔生物科技有限公司

IL-17A modulator-1

IL-17A modulator-1 Chemical Structure

CAS No. : 2748749-29-1

规格	价格	是否有货
5 mg	￥5800	询问价格 & 货期
10 mg	￥9200	询问价格 & 货期
25 mg	￥18500	询问价格 & 货期

* Please select Quantity before adding items.

生物活性

IC₅₀ & Target^[1]

IL-17A

8.2 (pIC₅₀)

分子量

561.63

Formula

C₃₃H₃₁N₅O₄

CAS 号

2748749-29-1

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]. Barrie Phillip MARTIN, et al. Preparation of amino acid amides as IL-17A modulators. WO2021239743 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

P-gp modulator 2

发表于2023年11月30日由上海金畔生物科技有限公司

P-gp modulator 2

P-gp modulator 2 (Compound 27) 是一种有效的竞争性和变构性 P-glycoprotein (P-gp) 调节剂。

P-gp modulator 2 Chemical Structure

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	P-gp modulator 2 (Compound 27) is a potent, competitive, allosteric P-glycoprotein (P-gp) modulator^[1].
体外研究 (In Vitro)	P-gp modulator 2 (Compound 27) shows cytotoxicity on L5178Y parental (L5178Y-PAR) and human ABCB1-gene transfected (L5178Y-MDR) mouse T-lymphoma cells with IC₅₀ values of 8.0 ± 1.1 and 10.7 ± 1.1 µM, respectively^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	470.32
Formula	C₂₂H₂₀BrN₃O₄
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]. Ferreira RJ, et al. Nitrogen-containing naringenin derivatives for reversing multidrug resistance in cancer. Bioorg Med Chem. 2020 Dec 1;28(23):115798.

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

P-gp modulator 3

发表于2023年11月30日由上海金畔生物科技有限公司

P-gp modulator 3

P-gp modulator 3 (Compound 37) 是一种有效的竞争性和变构性 P-glycoprotein (P-gp) 调节剂。

P-gp modulator 3 Chemical Structure

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	P-gp modulator 3 (Compound 37) is a potent, competitive, allosteric P-glycoprotein (P-gp) modulator^[1].
分子量	531.64
Formula	C₃₁H₃₇N₃O₅
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]. Ferreira RJ, et al. Nitrogen-containing naringenin derivatives for reversing multidrug resistance in cancer. Bioorg Med Chem. 2020 Dec 1;28(23):115798.

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P-gp modulator 1

发表于2023年8月12日由上海金畔生物科技有限公司

P-gp modulator 1

P-gp modulator 1 是一种高亲和力、口服有效的 p- 糖蛋白 (Pgp) 调节剂，可以逆转 Pgp 介导的多药抗性。

P-gp modulator 1 Chemical Structure

CAS No. : 2249749-39-9

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	P-gp modulator 1 is a high affinity, orally available modulator of P-glycoprotein (Pgp), can reverse the Pgp-mediated multidrug resistance ((MDR)^[1].
IC₅₀ & Target	P-glycoprotein
分子量	689.02
Formula	C₄₁H₇₂N₂O₆
CAS 号	2249749-39-9
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]. Ren Q, et al. Design, synthesis, and discovery of ocotillol-type amide derivatives as orally available modulators of P-glycoprotein-mediated multidrug resistance. Eur J Med Chem. 2019 Jan 1;161:118-130.

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IL-17 modulator 3

发表于2023年6月3日由上海金畔生物科技有限公司

IL-17 modulator 3

IL-17 modulator 3 是 IL-17 调节剂 (US20200247785A1)。IL-17 modulator 3 可用于炎症、癌症和自身免疫性疾病的研究。

IL-17 modulator 3 Chemical Structure

CAS No. : 2467731-88-8

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

IL-17 modulator 3 is an IL-17 modulator (US20200247785A1). IL-17 modulator 3 can be used for the research of inflammation, cancer and autoimmune diseases^[1].

IC₅₀ & Target^[1]

IL-17

分子量

579.73

Formula

C₃₁H₄₅N₇O₄

CAS 号

2467731-88-8

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]. Fatheree PR, et, al. IL-17 Ligands And Uses Thereof. US20200247785A1.

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