PNU-EDA-Gly5 是用于ADC 合成的低聚甘氨酸毒素分子偶联物,由 DNA 拓扑异构酶 I 抑制剂 PNU-159682 和 EDA-Gly5 里连接子组成。
PNU-EDA-Gly5 Chemical Structure
CAS No. : 1957223-28-7
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
PNU-EDA-Gly5 is an oligo-glycine linker-payload for ADC synthesis, composed of a DNA topoisomerase I inhibitor PNU-159682 and a linker EDA-Gly5[1].
分子量
954.93
Formula
C43H54N8O17
CAS 号
1957223-28-7
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]. Quintieri L, et al. Formation and antitumor activity of PNU-159682, a major metabolite of nemorubicin in human liver microsomes. Clin Cancer Res. 2005 Feb 15;11(4):1608-17.
PNU-EDA-Gly5 是用于ADC 合成的低聚甘氨酸毒素分子偶联物,由 DNA 拓扑异构酶 I 抑制剂 PNU-159682 和 EDA-Gly5 里连接子组成。
PNU-EDA-Gly5 Chemical Structure
CAS No. : 1957223-28-7
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
PNU-EDA-Gly5 is an oligo-glycine linker-payload for ADC synthesis, composed of a DNA topoisomerase I inhibitor PNU-159682 and a linker EDA-Gly5[1].
分子量
954.93
Formula
C43H54N8O17
CAS 号
1957223-28-7
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]. Quintieri L, et al. Formation and antitumor activity of PNU-159682, a major metabolite of nemorubicin in human liver microsomes. Clin Cancer Res. 2005 Feb 15;11(4):1608-17.
PNU-EDA-Gly5 是用于ADC 合成的低聚甘氨酸毒素分子偶联物,由 DNA 拓扑异构酶 I 抑制剂 PNU-159682 和 EDA-Gly5 里连接子组成。
PNU-EDA-Gly5 Chemical Structure
CAS No. : 1957223-28-7
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
PNU-EDA-Gly5 is an oligo-glycine linker-payload for ADC synthesis, composed of a DNA topoisomerase I inhibitor PNU-159682 and a linker EDA-Gly5[1].
分子量
954.93
Formula
C43H54N8O17
CAS 号
1957223-28-7
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]. Quintieri L, et al. Formation and antitumor activity of PNU-159682, a major metabolite of nemorubicin in human liver microsomes. Clin Cancer Res. 2005 Feb 15;11(4):1608-17.
N’-Boc-N-(Gly-Oleoyl)-Lys is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].
IC50 & Target
Alkyl-Chain
体外研究 (In Vitro)
PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
567.80
Formula
C31H57N3O6
CAS 号
2353409-71-7
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]. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562.
N’-Boc-N-(Gly-Oleoyl)-Lys is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].
IC50 & Target
Alkyl-Chain
体外研究 (In Vitro)
PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[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
567.80
Formula
C31H57N3O6
CAS 号
2353409-71-7
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]. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562.
N’-Boc-N-(Gly-Oleoyl)-Lys is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].
IC50 & Target
Alkyl-Chain
体外研究 (In Vitro)
PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
567.80
Formula
C31H57N3O6
CAS 号
2353409-71-7
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]. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562.
Arg-Gly-Glu-Ser is a RGD-related peptide and a control for the RGDS ihibitory activity on fibrinogen binding to activated platelets.
体内研究 (In Vivo)
Arg-Gly-Glu-Ser (5 mg/kg) in combination with LPS or saline + RGDS does not affect neutrophil and macrophage cell numbers and has no effect on protein accumulation compared with LPS- or saline-treated mice, 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.
分子量
447.44
Formula
C16H29N7O8
CAS 号
93674-97-6
Sequence
Arg-Gly-Glu-Ser
Sequence Shortening
RGES
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.
溶解性数据
In Vitro:
H2O : 2 mg/mL (4.47 mM; Need ultrasonic and warming)
配制储备液
浓度溶剂体积质量
1 mg
5 mg
10 mg
1 mM
2.2349 mL
11.1747 mL
22.3494 mL
5 mM
—
—
—
10 mM
—
—
—
参考文献
[1]. Moon C, et al. Synthetic RGDS peptide attenuates lipopolysaccharide-induced pulmonary inflammation by inhibiting integrin signaled MAP kinase pathways. Respir Res. 2009 Mar 9;10:18.
Animal Administration [1]
Mice[1] Mouse pharyngeal aspiration is performed in the assay. Animals are anesthetized with a mixture of ketamine and xylazine (45 mg/kg and 8 mg/kg, i.p., respectively). Test solution (30 μL) containing LPS (1.5 mg/kg) is placed posterior in the throat and aspirated into the lungs. Control mice are administrated sterile saline (0.9% NaCl). Animals are administered with RGDS or Arg-Gly-Glu-Ser peptide (1, 2.5 or 5 mg/kg, i.p.) once one hour before LPS treatment and sacrificed 4 h post-LPS. Animals are also administered RGDS or Arg-Gly-Glu-Ser peptide (5 mg/kg, i.p.) once at different time points (1 h before or 2 h after LPS treatment) and sacrificed 24 h post-LPS. In addition, animals are administered with αvβ3-blocking mAbs, anti-αv, or anti-β3 (5 mg/kg, i.p.) once 1 h before and sacrificed 4 h post-LPS. Animals administered with these mAbs 2 h after LPS treatment are sacrificed 24 h post-LPS[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]. Moon C, et al. Synthetic RGDS peptide attenuates lipopolysaccharide-induced pulmonary inflammation by inhibiting integrin signaled MAP kinase pathways. Respir Res. 2009 Mar 9;10:18.
Tyr-Gly-Gly-Phe-Met-OH regulates human immune function and inhibits tumor growth via binding to the opioid receptor.
IC50 & Target
Opioid Receptor[1].
体外研究 (In Vitro)
Methionine enkephalin (MENK), an endogenous neuropeptide has a crucial role in both neuroendocrine and immune systems. MENK is believed to have an immunoregulatory activity to have cancer biotherapy activity by binding to the opioid receptors on immune and cancer cells. MENK may also change the tumor microenvironment by binding to opioid receptor on or in cancer cells. All of these mechanisms of action have biologic significance and potential for use in cancer immunotherapy. Furthermore, they reveal a relationship between the endocrine and immune systems[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
573.66
Formula
C27H35N5O7S
CAS 号
58569-55-4
Sequence
Tyr-Gly-Gly-Phe-Met
Sequence Shortening
YGGFM
中文名称
蛋氨酸脑啡肽
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Zhao D, et al. Methionine enkephalin, its role in immunoregulation and cancer therapy. Int Immunopharmacol. 2016 Feb 23. pii: S1567-5769(16)30050-9.
Fmoc-Gly-Gly-D-Phe-OH is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Fmoc-Gly-Gly-D-Phe-OH is the D-isomer of Fmoc-Gly-Gly-Phe-OH (HY-131833).
IC50 & Target
Cleavable
体外研究 (In Vitro)
ADCs are comprised of an antibody to which is attached an ADC cytotoxin through an ADC linker[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
501.53
Formula
C28H27N3O6
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moisture and light
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)