多肽定制CB-TH 编码

发表于2024年4月19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可以定制不同序列多肽，可以访问官网了解更多产品信息。

名称	CB-TH
编码
别名	CB-TH
纯度	80%，90%，95%，98%，99%
重量	1mg,5mg,10mg,50mg,100mg,1g
序列（单字母缩写）	RWKIFKKIEKMGGSYCNRRTGKCQRM
序列（三字母缩写）	Arg-Trp-Lys-Ile-Phe-Lys-Lys-Ile-Glu-Lys-Met-Gly-Gly-Ser-Tyr-Cys-Asn-Arg-Arg-Thr-Gly-Lys-Cys-Gln-Arg-Met
基本描述
溶解度
分子量	3205.9
化学式	C138H230N46O34S4
存储条件	Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
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C端
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化学桥

Abiraterone-D4(Synonyms: CB-7598-D4)

发表于2024年4月9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。

Abiraterone-D4 (Synonyms: CB-7598-D4)

Abiraterone-D4 (CB-7598-D4) 是 Abiraterone 的氘代物。Abiraterone 是一种有效的不可逆的 CYP17A1 抑制剂，具有抗雄激素活性，抑制细胞色素 p450 酶 CYP17 的 17α-羟化酶和 17,20-裂合酶活性，IC₅₀ 值分别为 2.5 nM 和 15 nM.

Abiraterone-D4 Chemical Structure

CAS No. : 2122245-62-7

规格	价格	是否有货
1 mg	￥4300	询问价格 & 货期

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生物活性	Abiraterone-D4 (CB-7598-D4) is the deuterium labeled Abiraterone. Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, which inhibits both the 17α-hydroxylase and 17,20-lyase activity of the cytochrome p450 enzyme CYP17 with IC₅₀s of 2.5 nM and 15 nM, respectively.
体外研究 (In Vitro)	Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	353.53
Formula	C₂₄H₂₇D₄NO
CAS 号	2122245-62-7
中文名称	阿比特龙 D4
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]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [2]. Attard G, et al. Phase I clinical trial of a selective inhibitor of CYP17, abiraterone acetate, confirms that castration-resistant prostate cancer commonly remains hormone driven. J Clin Oncol. 2008 Oct 1;26(28):4563-71.;Richards J, et al. Interactions of abiraterone, eplerenone, and prednisolone with wild-type and mutant androgen receptor: a rationale for increasing abiraterone exposure or combining with MDV3100. Cancer Res. 2012 May 1;72(9):2176-82.;Stein MN, et al. Androgen synthesis inhibitors in the treatment of castration-resistant prostate cancer. Asian J Androl. 2014 May-Jun;16(3):387-400.;Li R, et al. Abiraterone inhibits 3β-hydroxysteroid dehydrogenase: a rationale for increasing drug exposure in castration-resistant prostate cancer. Clin Cancer Res. 2012 Jul 1;18(13):3571-9.;Kumar SV, et al. Validated RP-HPLC/UV method for the quantitation of abiraterone in rat plasma and its application to a pharmacokinetic study in rats. Biomed Chromatogr. 2013 Feb;27(2):203-7.;Stein MN, et al. Androgen synthesis inhibitors in the treatment of castration-resistant prostate cancer. Asian J Androl. 2014 May-Jun;16(3):387-400.

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生物活性分子抑制剂(-)-Indolactam V(Synonyms: Indolactam V)

发表于2024年4月6日由上海金畔生物科技有限公司

生物活性分子抑制剂特异性抑制剂激动剂化合物库重组蛋白 (-)-Indolactam V (Synonyms: Indolactam V) 纯度: 98.63%

(-)-Indolactam V 是 PKC 的激活剂，对 η-CRD2 (PKCη 代替肽)，γ-CRD2 (PKCγ 代替肽) 的 K_i 值分别为 3.36 nM 和 1.03 μM，对 PKC C1A 和 C1B 结构域的 K_d 值分别为 5.5 nM (η-C1B)，7.7 nM (ε-C1B)，8.3 nM (δ-C1B)，18.9 nM (β-C1A-long)，20.8 nM (α-C1A-long)，137 nM (β-C1B)，138 nM (γ-C1A) 和 213 nM (γ-C1B)，具有抗肿瘤活性。

(-)-Indolactam V Chemical Structure

CAS No. : 90365-57-4

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥4376	In-stock
1 mg	￥1800	In-stock
5 mg	￥6600	In-stock
10 mg		询价
50 mg		询价

* Please select Quantity before adding items.

(-)-Indolactam V 相关产品

•相关化合物库:

Bioactive Compound Library Plus

生物活性

(-)-Indolactam V is a PKC activator, with K_is of 3.36 nM, 1.03 μM for η-CRD2 (PKCη surrogate peptide), γ-CRD2 (PKCγ surrogate peptide), and K_ds of 5.5 nM (η-C1B), 7.7 nM (ε-C1B), 8.3 nM (δ-C1B), 18.9 nM (β-C1A-long), 20.8 nM (α-C1A-long), 137 nM (β-C1B), 138 nM (γ-C1A), 213 nM (γ-C1B), and has antitumor activity.

IC₅₀ & Target^[1]^[2]

PKCη-CRD2

3.36 nM (Ki)

PKCη-C1B

5.5 nM (Kd)

PKCε-C1B

7.7 nM (Kd)

PKCδ-C1B

8.3 nM (Kd)

PKCθ-C1B

8.7 nM (Kd)

PKCβ-C1A-long

18.9 nM (Kd)

PKCα-C1A-long

20.8 nM (Kd)

PKCβ-C1B

137 nM (Kd)

PKCγ-C1A

138 nM (Kd)

PKCγ-C1B

213 nM (Kd)

PKCγ-CRD2

1030 nM (Ki)

PKCδ-C1A

1900 nM (Kd)

PKCη-C1A

3770 nM (Kd)

PKCα-C1B-long

4000 nM (Kd)

PKCε-C1A

4110 nM (Kd)

体外研究
(In Vitro)

(-)-Indolactam V is a PKC activator, with K_is of 3.36 nM, 1.03 μM for η-CRD2 (PKCη surrogate peptide), γ-CRD2 (PKCγ surrogate peptide), and has antitumor activity^[1]. (-)-Indolactam V shows K_ds of 5.5 nM (η-C1B), 7.7 nM (ε-C1B), 8.3 nM (δ-C1B), 18.9 nM (β-C1A-long), 20.8 nM (α-C1A-long), 137 nM (β-C1B), 138 nM (γ-C1A), 213 nM (γ-C1B), respectively^[2]. (-)-Indolactam V (20 nM-5 μM) dose-dependently affects multiple hESC lines, such as HUES 2, 4 and 8. (-)-Indolactam V also increases the mRNA levels of Pdx1, HNF6, PTF1A, SOX9, HB9 and PROX1. In addition, (-)-Indolactam V (300 nM) functions in both mouse and human cells and confirms that some signals for pancreatic development^[3].

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

301.38

Formula

C₁₇H₂₃N₃O₂

CAS 号

90365-57-4

中文名称

吲哚内酰胺 V

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 : 50 mg/mL (165.90 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.3181 mL	16.5904 mL	33.1807 mL
5 mM	0.6636 mL	3.3181 mL	6.6361 mL
10 mM	0.3318 mL	1.6590 mL	3.3181 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: ≥ 2.5 mg/mL (8.30 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.30 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 (8.30 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.30 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 (8.30 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.30 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]. Nakagawa Y, et al. Synthesis and biological activities of indolactone-V, the lactone analogue of the tumor promoter (-)-indolactam-V. Biosci Biotechnol Biochem. 1997 Aug;61(8):1415-7.

[2]. Masuda A, et al. Binding selectivity of conformationally restricted analogues of (-)-indolactam-V to the C1 domains of protein kinase C isozymes. Biosci Biotechnol Biochem. 2002 Jul;66(7):1615-7.

[3]. Chen S, et al. A small molecule that directs differentiation of human ESCs into the pancreatic lineage. Nat Chem Biol. 2009 Apr;5(4):258-65.

Cell Assay ^[3]	For induced differentiation to endocrine or exocrine cells, the (-)-Indolactam V (300 nM)-treated populations are cultured in DMEM/F12 supplemented with 1 N₂, 2 mg/mL albumin fraction V and 10 ng/mL bovine FGF for the first 4 d. 10 mM nicotinamide is then added and maintained for an additional 8 d, changing the medium every 3 d^[3]. 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.
参考文献	[1]. Nakagawa Y, et al. Synthesis and biological activities of indolactone-V, the lactone analogue of the tumor promoter (-)-indolactam-V. Biosci Biotechnol Biochem. 1997 Aug;61(8):1415-7. [2]. Masuda A, et al. Binding selectivity of conformationally restricted analogues of (-)-indolactam-V to the C1 domains of protein kinase C isozymes. Biosci Biotechnol Biochem. 2002 Jul;66(7):1615-7. [3]. Chen S, et al. A small molecule that directs differentiation of human ESCs into the pancreatic lineage. Nat Chem Biol. 2009 Apr;5(4):258-65.

Cell Assay
^[3]

For induced differentiation to endocrine or exocrine cells, the (-)-Indolactam V (300 nM)-treated populations are cultured in DMEM/F12 supplemented with 1 N₂, 2 mg/mL albumin fraction V and 10 ng/mL bovine FGF for the first 4 d. 10 mM nicotinamide is then added and maintained for an additional 8 d, changing the medium every 3 d^[3].

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.

参考文献

[1]. Nakagawa Y, et al. Synthesis and biological activities of indolactone-V, the lactone analogue of the tumor promoter (-)-indolactam-V. Biosci Biotechnol Biochem. 1997 Aug;61(8):1415-7.

[2]. Masuda A, et al. Binding selectivity of conformationally restricted analogues of (-)-indolactam-V to the C1 domains of protein kinase C isozymes. Biosci Biotechnol Biochem. 2002 Jul;66(7):1615-7.

[3]. Chen S, et al. A small molecule that directs differentiation of human ESCs into the pancreatic lineage. Nat Chem Biol. 2009 Apr;5(4):258-65.

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Chlorambucil(Synonyms: CB-1348; WR-139013)

发表于2024年3月20日由上海金畔生物科技有限公司

Chlorambucil (Synonyms: CB-1348; WR-139013) 纯度: 98.76%

Chlorambucil 是一种口服抗肿瘤活性剂和双功能烷基化剂 (alkylating agent)，属于氮芥类。Chlorambucil 可用于研究淋巴细胞白血病、卵巢癌和乳腺癌以及霍奇金病。

Chlorambucil Chemical Structure

CAS No. : 305-03-3

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥1320	In-stock
100 mg	￥1200	In-stock
500 mg	￥3200	In-stock
1 g		询价
5 g		询价

* Please select Quantity before adding items.

Chlorambucil 相关产品

•相关化合物库:

Drug Repurposing Compound Library Plus
FDA-Approved Drug Library Plus
FDA-Approved Drug Library Mini
Bioactive Compound Library Plus
Cell Cycle/DNA Damage Compound Library
FDA-Approved Drug Library
Anti-Cancer Compound Library
CNS-Penetrant Compound Library
Anti-Aging Compound Library
Drug Repurposing Compound Library
Orally Active Compound Library
FDA Approved & Pharmacopeial Drug Library
Anti-Lung Cancer Compound Library
Drug-Induced Liver Injury (DILI) Compound Library
Anti-Blood Cancer Compound Library
Targeted Diversity Library
Tumorigenesis Related Compound Library
Rare Diseases Drug Library

生物活性

Chlorambucil (CB-1348), an orally active antineoplastic agent, is a bifunctional alkylating agent belonging to the nitrogen mustard group. Chlorambucil can be used for the research of lymphocytic leukemia, ovarian and breast carcinomas, and Hodgkin’s disease^[1]^[2]^[3]^[4].

IC₅₀ & Target

DNA Alkylator^[1]

体外研究
(In Vitro)

Chlorambucil can deprive the function of complementary strands of DNA molecules via alkalization-induced cross interaction, and then inhibits tumor cell proliferation. Chlorambucil (0, 2.5, 5, 10 μM) exhibits slight inhibitory effect on Raji cell apoptosis, but potently increases DR4 and DR5 mRNA expression in Raji cells. Chlorambucil (10 μM) in combination with Tumor necrosis factor (TNF) related apoptosis inducing ligand (TRAIL, 80 ng/ml) has synergistic effect on Raji cell apoptosis and inhibition on proliferation^[1].
Chlorambucil is a DNA alkylator at high doses and, at lower doses, acts as an inhibitor of synthesis of nuclear proteins, particularly histones. Increasing doses are associated with a higher frequency of apoptosis, whereas long-term maintenance therapy has been associated with mutations of the p53 gene, leading to secondary malignancies^[4].

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)

Chlorambucil (0.2 mg/kg, p.o.) in combination with levamisole (5 mg/kg) has enhanced anti-cancer effect on Ehrlich ascites carcinoma which elevates apoptosis of Ehrlich ascites carcinoma and the survival rate of the mice. However, Chlorambucil exhibits adverse effects on the liver and kidneys of mice^[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.

Clinical Trial

分子量

304.21

Formula

C₁₄H₁₉Cl₂NO₂

CAS 号

305-03-3

中文名称

苯丁酸氮芥；氯氨布布西；氯氨布西；瘤可宁；氯氨布西

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 : ≥ 24 mg/mL (78.89 mM)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.2872 mL	16.4360 mL	32.8720 mL
5 mM	0.6574 mL	3.2872 mL	6.5744 mL
10 mM	0.3287 mL	1.6436 mL	3.2872 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 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (8.22 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.22 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 (8.22 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.22 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 (8.22 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.22 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]. Guo JX, et al. Synergistic effects of chlorambucil and TRAIL on apoptosis and proliferation of Raji cells. Eur Rev Med Pharmacol Sci. 2017 Oct;21(20):4703-4710.

[2]. Salem FS, et al. Biochemical and pathological studies on the effects of levamisole and chlorambucil on Ehrlich ascites carcinoma-bearing mice. Vet Ital. 2011 Jan-Mar;47(1):89-95.

[3]. Mohamed D, et al. Chlorambucil-adducts in DNA analyzed at the oligonucleotide level using HPLC-ESI MS. Chem Res Toxicol. 2009;22(8):1435-1446.

[4]. Birnbaum AD, et al. Chlorambucil and malignancy. Ophthalmology. 2010;117(7):1466-1466.e1.

Cell Assay ^[1]	Cultured cells at log-growth phase are digested by trypsin into single cell suspension and are seeded into 96-well plate at 1000 per well density. The plate is placed in a 37°C chamber with 5% CO₂. After attached growth for 24 h, cells are treated with TRAIL at 0, 20, 40 and 80 ng/mL or Chlorambucil at 0, 2.5, 5 and 10 μM for 48 h. 10 μL CCK-8 reagent is added to each well, followed by incubation at 37°C for 4 h. Absorbance values at 450 nm are then measured by a micro-plate reader. Six parallel samples are performed in each treatment group. Cell proliferation rate (%) = mean value of experimental group/mean value of control group × 100%^[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 Administration ^[2]	Mice^[2] Female Swiss mice are divided randomly into five group (20 mice per group). Group 1 is kept as the control group, Group 2 receives intraperitoneal injection of by 2.5 × 10⁶ Ehrlich ascites carcinoma cell, Gropu 3 is treated orally with Chlorambucil 0.2 mg/kg body weight, Group 4 is treated orally with levamisole (5 mg/kg body weight) and Group 5 is treated orally with a combination of Chlorambucil and levamisole each day, using a bent stainless steel stomach tube^[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.
参考文献	[1]. Guo JX, et al. Synergistic effects of chlorambucil and TRAIL on apoptosis and proliferation of Raji cells. Eur Rev Med Pharmacol Sci. 2017 Oct;21(20):4703-4710. [2]. Salem FS, et al. Biochemical and pathological studies on the effects of levamisole and chlorambucil on Ehrlich ascites carcinoma-bearing mice. Vet Ital. 2011 Jan-Mar;47(1):89-95. [3]. Mohamed D, et al. Chlorambucil-adducts in DNA analyzed at the oligonucleotide level using HPLC-ESI MS. Chem Res Toxicol. 2009;22(8):1435-1446. [4]. Birnbaum AD, et al. Chlorambucil and malignancy. Ophthalmology. 2010;117(7):1466-1466.e1.

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

Tretazicar(Synonyms: CB 1954)

发表于2024年3月9日由上海金畔生物科技有限公司

Tretazicar (Synonyms: CB 1954) 纯度: 99.65%

Tretazicar (CB 1954) 是一种抗肿瘤前药，对 Walker 256 大鼠肿瘤细胞系具有很高的效力和选择性。Tretazicar 酶促活化后生成双功能试剂，该试剂可以形成 DNA-DNA 链间交联。大鼠细胞中的 Tretazicar 涉及通过酶 NAD(P)H：醌氧化还原酶1 (NQO1) 将其 4-硝基还原为 4-羟基胺。

Tretazicar Chemical Structure

CAS No. : 21919-05-1

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1387	In-stock
5 mg	￥800	In-stock
10 mg	￥1250	In-stock
50 mg		询价
100 mg		询价

* Please select Quantity before adding items.

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Anti-Lung Cancer Compound Library
Rare Diseases Drug Library

生物活性

Tretazicar (CB 1954), an antitumor prodrug, is highly selective against the Walker 256 rat tumour line. Tretazicar is enzymatically activated to generate a bifunctional agent, which can form DNA-DNA interstrand cross-links. Tretazicar in rat cells involves the reduction of its 4-nitro group to a 4-hydroxylamine by the enzyme NAD(P)H:quinone oxidoreductase 1 (NQO1)^[1]^[2].

体外研究
(In Vitro)

Tretazicar (CB 1954) (0.1-1000 μM; 3 days) has sensitivity for retrovirally transduced AB22 (AB22-nr) cells with an IC₅₀ of 3 μM^[3].
DNA cross-link formation in affected cells is a result of the bioactivation of the drug by the enzyme DT diaphorase (NAD(P)H dehydro-genase (quinone)) in the Walker cells which reduces the 4-nitro group of Tretazicar. The product of this reaction is a difunctional alkylating agent, 5-aziridin-1-yl-4-hydroxylamino-2-nitrobenzamide^[4].

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)

Tretazicar (CB 1954) (80 mg/kg; i.p. on days 2 and 9) results in a significant increase in survival^[3].

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:	Female BALB/c mice (AB22-nr, SKOV3 human ovarian tumour xenograft)^[3]
Dosage:	80 mg/kg
Administration:	i.p. on days 2 and 9
Result:	The median survival of the AB22-nr was 49 days. Resulted in a significant increase in survival.

分子量

252.18

Formula

C₉H₈N₄O₅

CAS 号

21919-05-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

溶解性数据

In Vitro:

DMSO : 125 mg/mL (495.68 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.9654 mL	19.8271 mL	39.6542 mL
5 mM	0.7931 mL	3.9654 mL	7.9308 mL
10 mM	0.3965 mL	1.9827 mL	3.9654 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 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.08 mg/mL (8.25 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (8.25 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 (8.25 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (8.25 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

*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]. Knox RJ,et al. Bioactivation of 5-(aziridin-1-yl)-2,4-dinitrobenzamide (CB 1954) by human NAD(P)H quinone oxidoreductase 2: a novel co-substrate-mediated antitumor prodrug therapy. Cancer Res. 2000 Aug 1;60(15):4179-86.

[2]. Knox RJ, et al. CB 1954: from the Walker tumor to NQO2 and VDEPT. Curr Pharm Des. 2003;9(26):2091-104.

[3]. Green NK, et al. Immune enhancement of nitroreductase-induced cytotoxicity: studies using a bicistronicadenovirus vector. Int J Cancer. 2003 Mar 10;104(1):104-12.

[4]. Drabek D, et al. The expression of bacterial nitroreductase in transgenic mice results in specific cell killing by the prodrug CB1954. Gene Ther. 1997 Feb;4(2):93-100.

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CB 300919

发表于2024年2月22日由上海金畔生物科技有限公司

CB 300919 纯度: 98.53%

CB 300919 是一种喹唑啉类抗肿瘤药物，在 CH1 人卵巢肿瘤异种移植中具有很高的活性。CB 300919 对人 CH1 卵巢癌外植体的 IC₅₀ 值为 2 nM。

CB 300919 Chemical Structure

CAS No. : 289715-28-2

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥3012	In-stock
5 mg	￥2344	In-stock
10 mg	￥4185	In-stock
50 mg	￥13950	In-stock
100 mg		询价
200 mg		询价

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CB 300919 相关产品

•相关化合物库:

Covalent Screening Library Plus
Bioactive Compound Library Plus
Metabolism/Protease Compound Library
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Covalent Screening Library

生物活性

CB 300919 is a quinazoline-based antitumour agent with high activity in the CH1 human ovarian tumour xenograft. CB 300919 has a continuous exposure (96 h) growth inhibition IC₅₀ value of 2 nM in human CH1 ovarian tumor xenograft^[1].

分子量

584.11

Formula

C₃₂H₃₄ClN₇O₂

CAS 号

289715-28-2

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 : ≥ 100 mg/mL (171.20 mM)

H₂O : < 0.1 mg/mL (insoluble)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7120 mL	8.5600 mL	17.1201 mL
5 mM	0.3424 mL	1.7120 mL	3.4240 mL
10 mM	0.1712 mL	0.8560 mL	1.7120 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 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 3 mg/mL (5.14 mM); Clear solution

此方案可获得 ≥ 3 mg/mL (5.14 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 30.0 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: 3 mg/mL (5.14 mM); Suspended solution; Need ultrasonic

此方案可获得 3 mg/mL (5.14 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 30.0 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: ≥ 3 mg/mL (5.14 mM); Clear solution

此方案可获得 ≥ 3 mg/mL (5.14 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 30.0 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]. Lockman JW, et al. Analogues of 4-[(7-Bromo-2-methyl-4-oxo-3H-quinazolin-6-yl)methylprop-2-ynylamino]-N-(3-pyridylmethyl)benzamide (CB-30865) as Potent Inhibitors of Nicotinamide Phosphoribosyltransferase (Nampt). J. Med. Chem., 2010, 53 (24), pp 8734-8746

[2]. Bavetsias, V. et al. The Design and Synthesis of Water-Soluble Analogues of CB30865, a Quinazolin-4-one-Based Antitumor Agent. Journal of Medicinal Chemistry (2002), 45(17), 3692-3702.

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CB30865(Synonyms: ZM 242421)

发表于2024年2月13日由上海金畔生物科技有限公司

CB30865 (Synonyms: ZM 242421) 纯度: 98.05%

CB30865 (ZM 242421) 是一种烟酰胺磷酸核糖转移酶 (Nampt) 抑制剂，具有很强的细胞毒性。CB30865 在体外能抑制多种人类肿瘤细胞系 (IC₅₀ 值在 1-10 nM 范围内)。

CB30865 Chemical Structure

CAS No. : 206275-15-2

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥3022	In-stock
5 mg	￥2660	In-stock
10 mg	￥3432	In-stock
50 mg	￥9263	In-stock
100 mg	￥13020	In-stock
200 mg		询价
500 mg		询价

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CB30865 相关产品

•相关化合物库:

Covalent Screening Library Plus
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Anti-Cancer Compound Library
Covalent Screening Library

生物活性

CB30865 (ZM 242421) is a nicotinamide phosphoribosyltransferase (Nampt) inhibitor, with potent cytotoxicity. CB30865 is highly potent against a variety of human tumour cell lines (IC₅₀ values in the 1-10 nM range)^[1]^[2].

体外研究
(In Vitro)

CB30865 exhibits cytotoxicity due to NAD reduction via Nampt 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.

分子量

516.39

Formula

C₂₆H₂₂BrN₅O₂

CAS 号

206275-15-2

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 : 33.33 mg/mL (64.54 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9365 mL	9.6826 mL	19.3652 mL
5 mM	0.3873 mL	1.9365 mL	3.8730 mL
10 mM	0.1937 mL	0.9683 mL	1.9365 mL

参考文献

[1]. Fleischer TC, et al. Chemical proteomics identifies Nampt as the target of CB30865, an orphan cytotoxic compound. Chem Biol. 2010 Jun 25;17(6):659-664.

[2]. Skelton LA, et al. Cell cycle effects of CB30865, a lipophilic quinazoline-based analogue of the antifolate thymidylate synthase inhibitor ICI 198583 with an undefined mechanism of action. Cytometry. 1998 Sep 1;33(1):56-66.

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Numidargistat(Synonyms: CB-1158; INCB01158)

发表于2024年2月11日由上海金畔生物科技有限公司

Numidargistat (Synonyms: CB-1158; INCB01158)

Numidargistat (CB-1158) 是一种有效的，具有口服活性的精氨酸酶 (arginase) 抑制剂，对重组人 arginase 1 和 arginase 2 的 IC₅₀ 值分别为 86 nM 和 296 nM。免疫肿瘤剂。

Numidargistat Chemical Structure

CAS No. : 2095732-06-0

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Numidargistat 的其他形式现货产品:

Numidargistat dihydrochloride

生物活性	Numidargistat (CB-1158) is a potent and orally active inhibitor of arginase, with IC₅₀s of 86 nM and 296 nM for recombinant human arginase 1 and recombinant human arginase 2, respectively. Immuno-oncology agent^[1].
IC₅₀ & Target	IC50: 86 nM (Arginase 1), 296 nM (Arginase 2)^[1]
体外研究 (In Vitro)	Numidargistat is a potent and orally-bioavailable inhibitor of arginase, with IC₅₀s of 86 and 296 nM for recombinant human arginase 1 and 2, respectively. Numidargistat inhibits native rginase 1 (Arg1) in human granulocyte, erythrocyte, and hepatocyte lysate with IC₅₀s of 178 nM, 116 nM and 158 nM, respectively, and blocks Arg1 in cancer patient plasma (IC₅₀, 122 nM). Numidargistat also exhibits potent inhibitory activity against arginase in human HepG2, K562 cell lines and primary human hepatocytes with IC₅₀s of 32, 139, 210 μM, respectively. Numidargistat show no effect on NOS. In addition, Numidargistat is not directly cytotoxic to murine cancer cell lines^[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)	Numidargistat (100 mg/kg, p.o., twice per day) increases the number of tumor-infiltrating cytotoxic cells and decreases myeloid cells in mice. Numidargistat in combination with PD-L1 blockade or gemcitabine inhibits tumor growth in mice bearing CT26 cancer cells^[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	287.12
Formula	C₁₁H₂₂BN₃O₅
CAS 号	2095732-06-0
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]. Steggerda SM, et al. Inhibition of arginase by CB-1158 blocks myeloid cell-mediated immune suppression in the tumor microenvironment. J Immunother Cancer. 2017 Dec 19;5(1):101.

Cell Assay ^[1]	Intracellular arginase activity is determined for the arginase-expressing HepG2 and K-562 cell lines as follows. HepG2 cells are seeded at 100,000 cells per well one day prior to treatment with CB-1158. K-562 cells are seeded at 200,000 cells per well on the day of CB-1158 treatment. Cells are treated with a dose-titration of CB-1158 in SILAC RPMI-1640 media containing 5% heat-inactivated and dialyzed FBS, antibiotics/anti-mycotic, 10 mM L-arginine, 0.27 mM L-lysine, and 2 mM L-glutamine. The medium is harvested after 24 h and urea generated is determined. Wells containing media without cells are used as background controls. For assessing the effect of CB-1158 on Arg1 in primary hepatocytes, frozen human hepatocytes are thawed, allowed to adhere onto collagen-coated wells for 4 h, and then incubated for 48 h in SILAC-RPMI containing 10 mM L-ornithine, no L-arginine, and a dose-titration of CB-1158, at which time the media are analyzed for urea^[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 Administration ^[1]	Mice^[1] For the 4T1 tumor model, 10⁵ cells are injected orthotopically into the mammary fat pad; for all other tumor models, 10⁶ cells are injected subcutaneously (s.c.) in the right flank. For all studies, CB-1158 is administered by oral gavage twice per day at 100 mg/kg starting on study day 1 (1 day after tumor implant). Control groups receive vehicle (water) twice daily by gavage. Tumor volume measured by digital caliper (length × width × width/2) and body weight are recorded three times per week. Mice are euthanized when tumors necrotize or volumes reach 2000 mm³. For the CT26 model, anti-PD-L1 antibody (5 mg/kg) is injected intraperitoneally (i.p.) on days 5, 7, 9, 11, 13, and 15. For the 4T1 model, anti-CTLA-4 antibody (5 mg/kg) is injected i.p. on days 2, 5, and 8; anti-PD-1 antibody (5 mg/kg) is injected i.p. on days 3, 6, and 9. 4T1 tumors are harvested on study day 25 into Fekete’s solution and tumor nodules are enumerated visually. Gemcitabine is dosed 50 mg/kg i.p. on days 10 and 16 for the CT26 model, 60 mg/kg i.p. on days 6 and 10 for the LLC model, or 30 mg/kg i.p. on day 5 for the 4T1 model. With these regimens, gemcitabine modestly reduces tumor growth and spares most tumor-infiltrating immune cells, allowing for the evaluation of combination activity with CB-1158^[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.
参考文献	[1]. Steggerda SM, et al. Inhibition of arginase by CB-1158 blocks myeloid cell-mediated immune suppression in the tumor microenvironment. J Immunother Cancer. 2017 Dec 19;5(1):101.

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尤尼柯C87B台式低速离心机

发表于2024年1月19日由上海金畔生物科技有限公司

尤尼柯C87B台式低速离心机

品牌尤尼柯|UNICO

型号 C87B

商品详情

产品特征

1、设有超速、不平衡门盖锁保护，确保人身、仪器运行安全

2、外壳采用了阻燃性ABS注塑成型

3、微机控制，多种程序设定，易操作

4、直流无刷电机,无碳粉污染

5、配有多种转子，方便用户选用

技术参数

产品型号	C87B
调速范围	500-5500r/min
最大相对离心力	4532×g
时间控制范围	1-99min
电源	AC220V50HZ
外形尺寸	350×380×290mm
净重	12KG

CB2 receptor agonist 3(Synonyms: GP2a)

发表于2023年12月28日由上海金畔生物科技有限公司

CB2 receptor agonist 3 (Synonyms: GP2a)

CB2 receptor agonist 3 是一种稳健和选择性的 CB2 大麻素激动剂，对 CB2 和 CB1 的 K_i 分别为 7.6 和 900 nM。CB2 receptor agonist 3 显著增加 HL-60 细胞 P-ERK1/2 的表达。

CB2 receptor agonist 3 Chemical Structure

CAS No. : 919077-81-9

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	CB2 receptor agonist 3 is a robust and selective CB2 cannabinoid agonist with K_is of 7.6 and 900 nM for CB2 and CB1, respectively. CB2 receptor agonist 3 significantly increases P-ERK 1/2 expression in HL-60 cells^[1].
体外研究 (In Vitro)	CB2 receptor agonist 3 (Compound 2a) is also shown to be agonist in an in vitro model based on human promyelocytic leukemia HL-60 cells^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	440.36
Formula	C₂₄H₂₃Cl₂N₃O
CAS 号	919077-81-9
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]. Murineddu G, et al. Tricyclic pyrazoles. 4. Synthesis and biological evaluation of analogues of the robust and selective CB2 cannabinoid ligand 1-(2′,4′-dichlorophenyl)-6-methyl-N-piperidin-1-yl-1,4-dihydroindeno[1,2-c]pyrazole-3-carboxamide. J Med Chem. 2006;49(25):7502-7512.

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CB2 receptor agonist 3(Synonyms: GP2a)

发表于2023年12月28日由上海金畔生物科技有限公司

CB2 receptor agonist 3 (Synonyms: GP2a)

CB2 receptor agonist 3 Chemical Structure

CAS No. : 919077-81-9

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	CB2 receptor agonist 3 is a robust and selective CB2 cannabinoid agonist with K_is of 7.6 and 900 nM for CB2 and CB1, respectively. CB2 receptor agonist 3 significantly increases P-ERK 1/2 expression in HL-60 cells^[1].
体外研究 (In Vitro)	CB2 receptor agonist 3 (Compound 2a) is also shown to be agonist in an in vitro model based on human promyelocytic leukemia HL-60 cells^[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	440.36
Formula	C₂₄H₂₃Cl₂N₃O
CAS 号	919077-81-9
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]. Murineddu G, et al. Tricyclic pyrazoles. 4. Synthesis and biological evaluation of analogues of the robust and selective CB2 cannabinoid ligand 1-(2′,4′-dichlorophenyl)-6-methyl-N-piperidin-1-yl-1,4-dihydroindeno[1,2-c]pyrazole-3-carboxamide. J Med Chem. 2006;49(25):7502-7512.

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CB2 receptor agonist 3(Synonyms: GP2a)

发表于2023年12月28日由上海金畔生物科技有限公司

CB2 receptor agonist 3 (Synonyms: GP2a)

CB2 receptor agonist 3 Chemical Structure

CAS No. : 919077-81-9

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	CB2 receptor agonist 3 is a robust and selective CB2 cannabinoid agonist with K_is of 7.6 and 900 nM for CB2 and CB1, respectively. CB2 receptor agonist 3 significantly increases P-ERK 1/2 expression in HL-60 cells^[1].
体外研究 (In Vitro)	CB2 receptor agonist 3 (Compound 2a) is also shown to be agonist in an in vitro model based on human promyelocytic leukemia HL-60 cells^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	440.36
Formula	C₂₄H₂₃Cl₂N₃O
CAS 号	919077-81-9
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]. Murineddu G, et al. Tricyclic pyrazoles. 4. Synthesis and biological evaluation of analogues of the robust and selective CB2 cannabinoid ligand 1-(2′,4′-dichlorophenyl)-6-methyl-N-piperidin-1-yl-1,4-dihydroindeno[1,2-c]pyrazole-3-carboxamide. J Med Chem. 2006;49(25):7502-7512.

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Chlorambucil-d8-1(Synonyms: CB-1348-d8-1; WR-139013-d8-1)

发表于2023年12月20日由上海金畔生物科技有限公司

Chlorambucil-d8-1 (Synonyms: CB-1348-d8-1; WR-139013-d8-1)

Chlorambucil-d8-1 (CB-1348-d8-1) 是 Chlorambucil 的氘代物。Chlorambucil 是一种口服抗肿瘤活性剂和双功能烷基化剂 (alkylating agent)，属于氮芥类。Chlorambucil 可用于研究淋巴细胞白血病、卵巢癌和乳腺癌以及霍奇金病。

Chlorambucil-d8-1 Chemical Structure

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生物活性	Chlorambucil-d8-1 (CB-1348-d8-1) is the deuterium labeled Chlorambucil. Chlorambucil (CB-1348), an orally active antineoplastic agent, is a bifunctional alkylating agent belonging to the nitrogen mustard group. Chlorambucil can be used for the research of lymphocytic leukemia, ovarian and breast carcinomas, and Hodgkin’s disease^[1]^[2]^[3]^[4].
体外研究 (In Vitro)	Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	312.26
Formula	C₁₄H₁₁D₈Cl₂NO₂
中文名称	苯丁酸氮芥 d8-1
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]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [2]. Guo JX, et al. Synergistic effects of chlorambucil and TRAIL on apoptosis and proliferation of Raji cells. Eur Rev Med Pharmacol Sci. 2017 Oct;21(20):4703-4710. [3]. Salem FS, et al. Biochemical and pathological studies on the effects of levamisole and chlorambucil on Ehrlich ascites carcinoma-bearing mice. Vet Ital. 2011 Jan-Mar;47(1):89-95. [4]. Mohamed D, et al. Chlorambucil-adducts in DNA analyzed at the oligonucleotide level using HPLC-ESI MS. Chem Res Toxicol. 2009;22(8):1435-1446. [5]. Birnbaum AD, et al. Chlorambucil and malignancy. Ophthalmology. 2010;117(7):1466-1466.e1.

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Chlorambucil-d8-1(Synonyms: CB-1348-d8-1; WR-139013-d8-1)

发表于2023年12月20日由上海金畔生物科技有限公司

Chlorambucil-d8-1 (Synonyms: CB-1348-d8-1; WR-139013-d8-1)

Chlorambucil-d8-1 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	Chlorambucil-d8-1 (CB-1348-d8-1) is the deuterium labeled Chlorambucil. Chlorambucil (CB-1348), an orally active antineoplastic agent, is a bifunctional alkylating agent belonging to the nitrogen mustard group. Chlorambucil can be used for the research of lymphocytic leukemia, ovarian and breast carcinomas, and Hodgkin’s disease^[1]^[2]^[3]^[4].
体外研究 (In Vitro)	Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	312.26
Formula	C₁₄H₁₁D₈Cl₂NO₂
中文名称	苯丁酸氮芥 d8-1
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]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [2]. Guo JX, et al. Synergistic effects of chlorambucil and TRAIL on apoptosis and proliferation of Raji cells. Eur Rev Med Pharmacol Sci. 2017 Oct;21(20):4703-4710. [3]. Salem FS, et al. Biochemical and pathological studies on the effects of levamisole and chlorambucil on Ehrlich ascites carcinoma-bearing mice. Vet Ital. 2011 Jan-Mar;47(1):89-95. [4]. Mohamed D, et al. Chlorambucil-adducts in DNA analyzed at the oligonucleotide level using HPLC-ESI MS. Chem Res Toxicol. 2009;22(8):1435-1446. [5]. Birnbaum AD, et al. Chlorambucil and malignancy. Ophthalmology. 2010;117(7):1466-1466.e1.

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Chlorambucil-d8-1(Synonyms: CB-1348-d8-1; WR-139013-d8-1)

发表于2023年12月20日由上海金畔生物科技有限公司

Chlorambucil-d8-1 (Synonyms: CB-1348-d8-1; WR-139013-d8-1)

Chlorambucil-d8-1 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	Chlorambucil-d8-1 (CB-1348-d8-1) is the deuterium labeled Chlorambucil. Chlorambucil (CB-1348), an orally active antineoplastic agent, is a bifunctional alkylating agent belonging to the nitrogen mustard group. Chlorambucil can be used for the research of lymphocytic leukemia, ovarian and breast carcinomas, and Hodgkin’s disease^[1]^[2]^[3]^[4].
体外研究 (In Vitro)	Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[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	312.26
Formula	C₁₄H₁₁D₈Cl₂NO₂
中文名称	苯丁酸氮芥 d8-1
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]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [2]. Guo JX, et al. Synergistic effects of chlorambucil and TRAIL on apoptosis and proliferation of Raji cells. Eur Rev Med Pharmacol Sci. 2017 Oct;21(20):4703-4710. [3]. Salem FS, et al. Biochemical and pathological studies on the effects of levamisole and chlorambucil on Ehrlich ascites carcinoma-bearing mice. Vet Ital. 2011 Jan-Mar;47(1):89-95. [4]. Mohamed D, et al. Chlorambucil-adducts in DNA analyzed at the oligonucleotide level using HPLC-ESI MS. Chem Res Toxicol. 2009;22(8):1435-1446. [5]. Birnbaum AD, et al. Chlorambucil and malignancy. Ophthalmology. 2010;117(7):1466-1466.e1.

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Chlorambucil-d8(Synonyms: CB-1348-d8; WR-139013-d8)

发表于2023年11月4日由上海金畔生物科技有限公司

Chlorambucil-d8 (Synonyms: CB-1348-d8; WR-139013-d8)

Chlorambucil-d8 (CB-1348-d8) 是 Chlorambucil 的氘代物。Chlorambucil 是一种口服抗肿瘤活性剂和双功能烷基化剂 (alkylating agent)，属于氮芥类。Chlorambucil 可用于研究淋巴细胞白血病、卵巢癌和乳腺癌以及霍奇金病。

Chlorambucil-d8 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	Chlorambucil-d8 (CB-1348-d8) is the deuterium labeled Chlorambucil. Chlorambucil (CB-1348), an orally active antineoplastic agent, is a bifunctional alkylating agent belonging to the nitrogen mustard group. Chlorambucil can be used for the research of lymphocytic leukemia, ovarian and breast carcinomas, and Hodgkin’s disease^[1]^[2]^[3]^[4].
体外研究 (In Vitro)	Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	312.26
Formula	C₁₄H₁₁D₈Cl₂NO₂
中文名称	苯丁酸氮芥 d8
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]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [2]. Guo JX, et al. Synergistic effects of chlorambucil and TRAIL on apoptosis and proliferation of Raji cells. Eur Rev Med Pharmacol Sci. 2017 Oct;21(20):4703-4710. [3]. Salem FS, et al. Biochemical and pathological studies on the effects of levamisole and chlorambucil on Ehrlich ascites carcinoma-bearing mice. Vet Ital. 2011 Jan-Mar;47(1):89-95. [4]. Mohamed D, et al. Chlorambucil-adducts in DNA analyzed at the oligonucleotide level using HPLC-ESI MS. Chem Res Toxicol. 2009;22(8):1435-1446. [5]. Birnbaum AD, et al. Chlorambucil and malignancy. Ophthalmology. 2010;117(7):1466-1466.e1.

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Telaglenastat(Synonyms: CB-839)

发表于2023年11月2日由上海金畔生物科技有限公司

Telaglenastat (Synonyms: CB-839) 纯度: 99.82%

Telaglenastat (CB-839) 是一种首创的，选择性的，可逆性的，口服活性的谷氨酰胺酶 1 (GLS1) 抑制剂。Telaglenastat 抑制 GLS1 剪接变异体 KGA 和 GAC，比 GLS2 具有更高的选择性。Telaglenastat 对小鼠类肾和脑中的内源性谷氨酰胺酶的 IC₅₀ 值分别为 23 nM 和 28 nM。Telaglenastat 还可诱导细胞自噬 (autophagy)，并具有强大的抗肿瘤活性。

Telaglenastat Chemical Structure

CAS No. : 1439399-58-2

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥1383	In-stock
2 mg	￥600	In-stock
5 mg	￥900	In-stock
10 mg	￥1500	In-stock
50 mg	￥4500	In-stock
100 mg	￥6750	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

Telaglenastat 相关产品

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Anti-Cancer Metabolism Compound Library
Mitochondria-Targeted Compound Library

生物活性

Telaglenastat (CB-839) is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC₅₀s are 23 nM and 28 nM for endogenous glutaminase in mouse kidney and brain, respectively. Telaglenastat inudces autophagy and has antitumor activity^[1].

IC₅₀ & Target

IC50: 23 nM (GLS1 in kidney), 28 nM (GLS1 in brain), >1 μM (GLS2 in liver)^[1]

体外研究
(In Vitro)

Telaglenastat (CB-839) (0.1-1000 nM; 72 hours) has antiproliferative activity in HCC1806 and MDA-MB-231 cells with IC₅₀s of 49 nM and 26 nM, respectively^[1].
Telaglenastat (CB-839) (1 μM; 72 hours) activates caspase 3/7 and induces apoptosis in MDA-MB-231 and HCC1806 cells^[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:	HCC1806, MDA-MB-231 cells
Concentration:	0.1, 1, 10, 100, 1000 nM
Incubation Time:	72 hours
Result:	Has a potent effect on the proliferation of the two TNBC cell lines (IC₅₀ of 49 nM and 26 nM for HCC1806 and MDA-MB-231 cells).

Apoptosis Analysis^[1]

Cell Line:	MDA-MB-231, HCC1806 cells
Concentration:	1 μM
Incubation Time:	72 hours
Result:	Caspase 3/7 activation.

体内研究
(In Vivo)

Telaglenastat (CB-839) (200 mg/kg; p.o.; twice daily for 28 days) has antitumor activity in xenograft models of TNBC^[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:	Female nu/nu mice with age 4–6 weeks (TNBC patient-derived xenograft model)^[1]
Dosage:	200 mg/kg
Administration:	Oral administration; twice daily for 28 days
Result:	Suppressed tumor growth by 61% relative to vehicle control at the end of study.

Clinical Trial

分子量

571.57

Formula

C₂₆H₂₄F₃N₇O₃S

CAS 号

1439399-58-2

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 : 6.29 mg/mL (11.00 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7496 mL	8.7478 mL	17.4957 mL
5 mM	0.3499 mL	1.7496 mL	3.4991 mL
10 mM	0.1750 mL	0.8748 mL	1.7496 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： 20% HP-β-CD/10 mM citrate pH 2.0

Solubility: 10 mg/mL (17.50 mM); Clear solution; Need ultrasonic
2.

请依序添加每种溶剂： 20% SBE-β-CD/10 mM Trisodium citrate adjusted to pH 2.0 with HCL

Solubility: 5 mg/mL (8.75 mM); Clear solution; Need ultrasonic and adjust pH to 2 with 1M HCl and heat to 55°C
3.

请依序添加每种溶剂： 70% PEG300 30% (20% SBE-β-CD in saline)

Solubility: 4 mg/mL (7.00 mM); Suspended solution; Need ultrasonic and warming and heat to 55°C

*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]. Gross MI, et al. Antitumor activity of the glutaminase inhibitor CB-839 in triple-negative breast cancer. Mol Cancer Ther. 2014 Apr;13(4):890-901.

[2]. Biancur DE, et al. Compensatory metabolic networks in pancreatic cancers upon perturbation of glutaminemetabolism. Nat Commun. 2017 Jul 3;8:15965.

[3]. Zhou WJ, et al. Estrogen inhibits autophagy and promotes growth of endometrial cancer by promoting glutamine metabolism. Cell Commun Signal. 2019 Aug 20;17(1):99.

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Glutaminase-IN-1(Synonyms: CB839 derivative)

发表于2023年10月30日由上海金畔生物科技有限公司

Glutaminase-IN-1 (Synonyms: CB839 derivative) 纯度: 98.65%

Glutaminase-IN-1 (CB839 derivative) 是CB839 的一个衍生物，是1,3,4-硒二氮基肾型谷氨酰胺酶(KGA) 的变构抑制剂，其IC₅₀ 值为1 nM。Glutaminase-IN-1 (CB839 derivative) 具有提高细胞摄取和抗肿瘤的活性。

Glutaminase-IN-1 Chemical Structure

CAS No. : 2247127-79-1

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥1633	In-stock
5 mg	￥1200	In-stock
10 mg	￥1900	In-stock
50 mg	￥5500	In-stock
100 mg	￥8500	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

Glutaminase-IN-1 相关产品

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Bioactive Compound Library Plus
Metabolism/Protease Compound Library
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生物活性

Glutaminase-IN-1 (CB839 derivative), a CB839 derivative, is an allosteric inhibitor of 1,3,4-selenadiazole-containing kidney-type glutaminase (KGA), with an IC₅₀ of 1 nM. Glutaminase-IN-1 (CB839 derivative) shows improved cellular uptake and antitumor activity.

IC₅₀ & Target

IC50: 1 nM (KGA)^[1].

体外研究
(In Vitro)

Glutaminase-IN-1 (CPD20), a CB839 derivative, is an allosteric inhibitor of 1,3,4-selenadiazole-containing kidney-type glutaminase (KGA), with an IC₅₀ of 1 nM. Glutaminase-IN-1 shows improved cellular uptake and antitumor activity. The IC₅₀ values of Glutaminase-IN-1 are 17 nM, 6.78 μM, 19 nM and 9 nM in A549, H2, Caki-1 and HCT116 cell lines, respectively. Glutaminase-IN-1 has better KGA inhibitory activity than the corresponding BPTES and CB839^[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)

Glutaminase-IN-1(10 mg/kg, s.c.) reduced the size and weight of the HCT116 tumor, and statistical analysis showed that the 40% reduction in tumor weight by CPD20 is statistically significant. Glutaminase-IN-1 could statistically significantly prolong the survival of H22-bearing 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

618.47

Formula

C₂₆H₂₄F₃N₇O₃Se

CAS 号

2247127-79-1

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 : 125 mg/mL (202.11 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (insoluble)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6169 mL	8.0845 mL	16.1689 mL
5 mM	0.3234 mL	1.6169 mL	3.2338 mL
10 mM	0.1617 mL	0.8084 mL	1.6169 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% corn oil

Solubility: ≥ 2.08 mg/mL (3.36 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.36 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。
2.

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

Solubility: ≥ 1.44 mg/mL (2.33 mM); Clear solution

此方案可获得 ≥ 1.44 mg/mL (2.33 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 14.4 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]. Chen Z, et al. Novel 1,3,4-Selenadiazole Containing Kidney-Type Glutaminase Inhibitors Showed Improved Cellular Uptake and Antitumor Activity. J Med Chem. 2018 Dec 13.

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CB-5083

发表于2023年10月29日由上海金畔生物科技有限公司

CB-5083 纯度: 99.90%

CB-5083 是一种首创的，有效的，具有口服活性的，选择性 p97 AAA ATPase/VCP 抑制剂。CB-5083 抑制 p97 AAA ATP 酶结构域 D2，IC₅₀ 为 11 nM。

CB-5083 Chemical Structure

CAS No. : 1542705-92-9

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥591	In-stock
2 mg	￥500	In-stock
5 mg	￥650	In-stock
10 mg	￥1100	In-stock
50 mg	￥2950	In-stock
100 mg	￥5300	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

CB-5083 相关产品

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生物活性

CB-5083 is a first-in-class, potent, selective, and orally bioavailable inhibitor of the p97 AAA ATPase/VCP. CB-5083 selectively inhibits p97 through its D2 site with the IC₅₀ of 11 nM^[1]。

IC₅₀ & Target

IC50: 11 nM (p97)^[1]

体外研究
(In Vitro)

CB-5083 shows cell killing potency with IC₅₀s of 0.68, 0.68, 1.03, and 0.49 μM for lung carcinoma A549 CTG, A549 K48, A549 CHOP, and A549 p62, respectively^[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)

CB-5083 (75 mg/kg; oral administration; qd; for 2 weeks) shows antitumor activity in an HCT 116 tumor xenograft model^[1].
CB-5083 exhibits terminal elimination half-life (T_1/2=2.56 h), moderate oral bioavailability (mouse 41%) and C_max (mouse 7.95 μM) following oral administration (25 mg/kg) in female nude mice^[1].
CB-5083 exhibits terminal elimination half-life (T_1/2=2.83 h) due to high plasma clearance (5.9 mL/min/kg respectively) combined with large volumes of distribution (418 mL/kg respectively) following intravenous administration (3.0 mg/kg) in female nude mice^[1].
CB-5083 has good metabolic stability with a 102 min T_1/2 in a mouse liver microsomal stability study and a 172 min T_1/2 in a hepatocyte stability study^[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:	Nu/Nu nude female mice bearing established human tumor xenografts derived from HCT 116 colon^[1]
Dosage:	75 mg/kg
Administration:	Administered orally using every day (qd) dosing, for 2 weeks.
Result:	Showed more profound antitumor activity.

Clinical Trial

分子量

413.47

Formula

C₂₄H₂₃N₅O₂

CAS 号

1542705-92-9

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 (241.86 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4186 mL	12.0928 mL	24.1856 mL
5 mM	0.4837 mL	2.4186 mL	4.8371 mL
10 mM	0.2419 mL	1.2093 mL	2.4186 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： 50% PEG300 50% saline

Solubility: 10 mg/mL (24.19 mM); Clear solution; Need ultrasonic
2.

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

Solubility: ≥ 2.5 mg/mL (6.05 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.05 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
3.

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

Solubility: ≥ 2.5 mg/mL (6.05 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.05 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
4.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (6.05 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.05 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]. Zhou HJ, et al. Discovery of a First-in-Class, Potent, Selective, and Orally Bioavailable Inhibitor of the p97 AAA ATPase (CB-5083). J Med Chem. 2015 Dec 24;58(24):9480-97.

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CB1151

发表于2023年10月27日由上海金畔生物科技有限公司

CB1151 纯度: ≥95.0%

CB1151 是 1,25 二羟基维生素D3 (VD) 的 20 表位类似物 ( 20-epi analogue of VD)，具有有效的抗肿瘤作用。CB1151 抑制 MCF-7 细胞生长， IC₅₀ 值为 0.82 nM。

CB1151 Chemical Structure

CAS No. : 182369-28-4

规格	价格	是否有货
1 mg	￥5000	In-stock
5 mg		询价
10 mg		询价

* Please select Quantity before adding items.

CB1151 相关产品

•相关化合物库:

Bioactive Compound Library Plus

生物活性

CB1151 is a 20-epi analogue of 1,25 dihydroxyvitamin D3 (VD) with potent anti-tumor effects. CB1151 inhibits MCF-7 cell growth with an IC₅₀ value of 0.82 nM^[1].

IC₅₀ & Target

IC50: 0.82 nM^[1]

体外研究
(In Vitro)

CB1151 (0-100 nM; 5 days) inhibits MCF-7 cells growth, this cell proliferation is accessed by [³H]-thymidine incorporation, exhibits an IC₅₀ value of 0.82 nM^[1].
CB1151 (0-100 nM; 40 hours) exhibits activation of the IP9-type VD response element with a EC₅₀ of 1.2 nM, the activation of IP9-type VD response elements shows a good correlation with inhibition of proliferation than the activation of DR3-type elements (EC₅₀=3.2nM) in MCF-7 cells transfected with the CAT reporter^[1].
CB1151 shows a functional dissociation constant (K_df) value of 3.6 nM. The ligand concentration that provides 50% of protease-resistant VDR fragment is defined by K_df, this is different from that of the traditional dissociation constant (K_d)^[2].

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

Cell Proliferation Assay^[1]

Cell Line:	MCF-7 cell
Concentration:	0 nM; 0.1nM; 0.5nM; 0.8nM; 1nM; 5nM; 10 nM
Incubation Time:	5 days
Result:	Inhibits MCF-7 cells growth.

分子量

446.66

Formula

C₂₈H₄₆O₄

CAS 号

182369-28-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light, stored under nitrogen

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

参考文献

[1]. Mørk Hansen C, et al. The potent anti-proliferative effect of 20-epi analogues of 1,25 dihydroxyvitamin D3 in human breast-cancer MCF-7 cells is related to promoter selectivity.Int J Cancer. 1996 Sep 4;67(5):739-42.

[2]. Nayeri S, et al. High-affinity nuclear receptor binding of 20-epi analogues of 1,25-dihydroxyvitamin D3 correlates well with gene activation.J Cell Biochem. 1996 Sep 1;62(3):325-33.

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