BRD4 ligand-Linker Conjugate 1 is a target protein ligand-linker conjugate that can be used in the synthesis of PROTACs.
分子量
500.04
Formula
C28H30ClN7
CAS 号
2154358-89-9
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]. Sun D, et al. Evaluation of the Small-molecule BRD4 Degrader CFT-2718 in Small-cell Lung Cancer and Pancreatic Cancer Models. Mol Cancer Ther. 2021 Aug;20(8):1367-1377.
BRD4 ligand-Linker Conjugate 1 is a target protein ligand-linker conjugate that can be used in the synthesis of PROTACs.
分子量
500.04
Formula
C28H30ClN7
CAS 号
2154358-89-9
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]. Sun D, et al. Evaluation of the Small-molecule BRD4 Degrader CFT-2718 in Small-cell Lung Cancer and Pancreatic Cancer Models. Mol Cancer Ther. 2021 Aug;20(8):1367-1377.
BRD4 ligand-Linker Conjugate 1 is a target protein ligand-linker conjugate that can be used in the synthesis of PROTACs.
分子量
500.04
Formula
C28H30ClN7
CAS 号
2154358-89-9
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]. Sun D, et al. Evaluation of the Small-molecule BRD4 Degrader CFT-2718 in Small-cell Lung Cancer and Pancreatic Cancer Models. Mol Cancer Ther. 2021 Aug;20(8):1367-1377.
Eicosanedioic acid is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Eicosanedioic acid is also a alkyl chain-based PROTAC linker that can be used in the synthesis
IC50 & Target
Non-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]. 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[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
342.51
Formula
C20H38O4
CAS 号
2424-92-2
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
参考文献
[1]. Beck A, et al. Strategies and challenges for the next generation of antibody-drug conjugates. Nat Rev Drug Discov. 2017;16(5):315-337.
[2]. Nalawansha DA, et al. PROTACs: An Emerging Therapeutic Modality in Precision Medicine. Cell Chem Biol. 2020;27(8):998-985.
Eicosanedioic acid is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Eicosanedioic acid is also a alkyl chain-based PROTAC linker that can be used in the synthesis
IC50 & Target
Non-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]. 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[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
342.51
Formula
C20H38O4
CAS 号
2424-92-2
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
参考文献
[1]. Beck A, et al. Strategies and challenges for the next generation of antibody-drug conjugates. Nat Rev Drug Discov. 2017;16(5):315-337.
[2]. Nalawansha DA, et al. PROTACs: An Emerging Therapeutic Modality in Precision Medicine. Cell Chem Biol. 2020;27(8):998-985.
Docosanedioic acid is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Docosanedioic acid is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1][2].
IC50 & Target
Non-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]. 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[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
370.57
Formula
C22H42O4
CAS 号
505-56-6
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
参考文献
[1]. Beck A, et al. Strategies and challenges for the next generation of antibody-drug conjugates. Nat Rev Drug Discov. 2017;16(5):315-337.
[2]. Nalawansha DA, et al. PROTACs: An Emerging Therapeutic Modality in Precision Medicine. Cell Chem Biol. 2020;27(8):998-985.
Docosanedioic acid is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Docosanedioic acid is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1][2].
IC50 & Target
Non-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]. 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[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
370.57
Formula
C22H42O4
CAS 号
505-56-6
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
参考文献
[1]. Beck A, et al. Strategies and challenges for the next generation of antibody-drug conjugates. Nat Rev Drug Discov. 2017;16(5):315-337.
[2]. Nalawansha DA, et al. PROTACs: An Emerging Therapeutic Modality in Precision Medicine. Cell Chem Biol. 2020;27(8):998-985.
AEEA-AEEA is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). AEEA-AEEA is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1][2].
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]. 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[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
308.33
Formula
C12H24N2O7
CAS 号
1143516-05-5
运输条件
Room temperature in continental US; may vary elsewhere.
Eicosanedioic acid is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Eicosanedioic acid is also a alkyl chain-based PROTAC linker that can be used in the synthesis
IC50 & Target
Non-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]. 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[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.
分子量
342.51
Formula
C20H38O4
CAS 号
2424-92-2
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
参考文献
[1]. Beck A, et al. Strategies and challenges for the next generation of antibody-drug conjugates. Nat Rev Drug Discov. 2017;16(5):315-337.
[2]. Nalawansha DA, et al. PROTACs: An Emerging Therapeutic Modality in Precision Medicine. Cell Chem Biol. 2020;27(8):998-985.
AEEA-AEEA is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). AEEA-AEEA is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1][2].
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]. 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[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
308.33
Formula
C12H24N2O7
CAS 号
1143516-05-5
运输条件
Room temperature in continental US; may vary elsewhere.
Docosanedioic acid is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Docosanedioic acid is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1][2].
IC50 & Target
Non-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]. 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[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.
分子量
370.57
Formula
C22H42O4
CAS 号
505-56-6
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
参考文献
[1]. Beck A, et al. Strategies and challenges for the next generation of antibody-drug conjugates. Nat Rev Drug Discov. 2017;16(5):315-337.
[2]. Nalawansha DA, et al. PROTACs: An Emerging Therapeutic Modality in Precision Medicine. Cell Chem Biol. 2020;27(8):998-985.
AEEA-AEEA is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). AEEA-AEEA is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1][2].
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]. 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[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.
分子量
308.33
Formula
C12H24N2O7
CAS 号
1143516-05-5
运输条件
Room temperature in continental US; may vary elsewhere.
1-N-Boc-3-hydroxyazetidine is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). 1-N-Boc-3-hydroxyazetidine is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs
IC50 & Target
Non-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]. 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[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
173.21
Formula
C8H15NO3
CAS 号
141699-55-0
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
参考文献
[1]. Beck A, et al. Strategies and challenges for the next generation of antibody-drug conjugates. Nat Rev Drug Discov. 2017;16(5):315-337.
[2]. Nalawansha DA, et al. PROTACs: An Emerging Therapeutic Modality in Precision Medicine. Cell Chem Biol. 2020;27(8):998-985.
1-N-Boc-3-hydroxyazetidine is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). 1-N-Boc-3-hydroxyazetidine is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs
IC50 & Target
Non-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]. 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[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
173.21
Formula
C8H15NO3
CAS 号
141699-55-0
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
参考文献
[1]. Beck A, et al. Strategies and challenges for the next generation of antibody-drug conjugates. Nat Rev Drug Discov. 2017;16(5):315-337.
[2]. Nalawansha DA, et al. PROTACs: An Emerging Therapeutic Modality in Precision Medicine. Cell Chem Biol. 2020;27(8):998-985.
1-N-Boc-3-hydroxyazetidine is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). 1-N-Boc-3-hydroxyazetidine is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs
IC50 & Target
Non-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]. 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[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.
分子量
173.21
Formula
C8H15NO3
CAS 号
141699-55-0
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
参考文献
[1]. Beck A, et al. Strategies and challenges for the next generation of antibody-drug conjugates. Nat Rev Drug Discov. 2017;16(5):315-337.
[2]. Nalawansha DA, et al. PROTACs: An Emerging Therapeutic Modality in Precision Medicine. Cell Chem Biol. 2020;27(8):998-985.
NAMPT inhibitor-linker 2 is a drug-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-4 consists of an NAMPT inhibitor-linker 2 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526, with IC50s of <7 pM and 40 pM, respectively.
IC50 & Target
Traditional Cytotoxic Agents
体外研究 (In Vitro)
ADC-4 exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526, with IC50s of <7 pm and 40 pm, respectively[1]. ADC-4 (0.01 nM-10 nM, 144 hours) inhibits cell proliferation of GIST-T1 cells, but does not affect the cell cycle[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:
GIST-T1 cells
Concentration:
0.1 pM-10 nM
Incubation Time:
144 hours
Result:
Inhibited the cell proliferation of GIST-T1 cells at 0.01-10 nM, and the inhibition remained unchanged after 1 nM.
体内研究 (In Vivo)
ADC-4 (20 mg/kg, i.v. for 28 days) is tolerated, and causes tumor stasis in mice bearing GIST-T1 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.
Animal Model:
Female scid-beige (SCID bg) mice[1]
Dosage:
20 mg/kg
Administration:
A single intravenous injection (i.v.) for 28 days
Result:
Significantly inhibited the growth of tumor in mice.
分子量
624.66
Formula
C34H33FN6O5
CAS 号
2241014-82-2
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]. Karpov AS, et al. Nicotinamide Phosphoribosyltransferase Inhibitor as a Novel Payload for Antibody-Drug Conjugates. ACS Med Chem Lett. 2018 Jun 28;9(8):838-842.
Thalidomide-O-amido-C8-NH2 (Cereblon Ligand-Linker Conjugates 2), a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker, can be used in the synthesis of PROTACs[1].
IC50 & Target[1]
Cereblon
体外研究 (In Vitro)
Thalidomide-O-amido-C8-NH2 is a degron-linker (refer to Compound DL7-TL). The PROTAC linker is bound lo at least one targeting ligand. Degron-linker-targeting ligand, wherein the linker is covalently bound lo at least one degron and at least one targeting ligand, the degron is a compound capable of binding to an ubiquitin ligase such as an E3 ubiquitin ligase (e g, cereblon), and the targeting ligand is capable of binding to the targeted protein (s)[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
458.51
Formula
C23H30N4O6
CAS 号
1950635-15-0
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]. James Bradner, et al. Methods to induce targeted protein degradation through bifunctional molecules. WO 2017024317 A2.
