Toxins for Antibody-Drug Conjugate Research Library
生物活性
SG3199 is a cytotoxic DNA minor groove interstrand crosslinking pyrrolobenzodiazepine (PBD) dimer. SG3199 is the released warhead component of the ADC payload Tesirine (SG3249)[1][2].
IC50 & Target[1]
Pyrrolobenzodiazepines
体外研究 (In Vitro)
SG3199 is potently cytotoxic against a panel of human solid tumour and haematological cancer cell lines with a mean GI50 of 151.5 pM. Cells defective in DNA repair protein ERCC1 or homologous recombination repair show increased sensitivity to SG3199 and the drug is only moderately susceptible to multidrug resistance mechanisms[1]. SG3199 is highly efficient at producing DNA interstrand cross-links in naked linear plasmid DNA and dose-dependent cross-linking is observed in 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.
体内研究 (In Vivo)
The in vitro binding of [3H]-SG3199 to the plasma proteins of rat (Sprague Dawley), cynomolgus monkey and human at concentrations of 0.8, 5 and 50 ng/mL is determined. Plasma protein binding is high in all species; rat ∼97%, cynomolgus monkey ∼90% and human ∼95%[1]. Following i.v. administration at 0.1 μg/kg, 0.5 μg/kg and 1 μg/kg, SG3199 shows a very rapid clearance in rats. In the 0.5 μg/kg and 1 μg/kg dose groups, the rapid clearance was between 1000 and 1500 mL/h/kg, with a T1/2 between 8 and 42 minutes[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
584.66
Formula
C33H36N4O6
CAS 号
1595275-71-0
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°C, protect from light, stored under nitrogen
*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
溶解性数据
In Vitro:
DMSO : 130 mg/mL (222.35 mM; Need ultrasonic)
配制储备液
浓度溶剂体积质量
1 mg
5 mg
10 mg
1 mM
1.7104 mL
8.5520 mL
17.1040 mL
5 mM
0.3421 mL
1.7104 mL
3.4208 mL
10 mM
0.1710 mL
0.8552 mL
1.7104 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, stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
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]. John A Hartley, et al. Pre-clinical pharmacology and mechanism of action of SG3199, the pyrrolobenzodiazepine (PBD) dimer warhead component of antibody-drug conjugate (ADC) payload tesirine. Sci Rep. 2018 Jul 11;8(1):10479.
[2]. Francesca Zammarchi, et al. ADCT-402, a PBD dimer-containing antibody drug conjugate targeting CD19-expressing malignancies. Blood. 2018 Mar 8;131(10):1094-1105.
Tesirine (SG3249) is an antibody-drug conjugate (ADC) pyrrolobenzodiazepine (PBD) dimer payload. Tesirine combines potent antitumor activity with desirable physicochemical properties such as favorable hydrophobicity and improved conjugation characteristics. SG3199 (HY-101161) is the released warhead component of the ADC payload Tesirine. SG3199 retains picomolar activity in a panel of cancer cell lines. PBD dimers are highly efficient DNA minor groove cross-linking agents with potent cytotoxicity[1][2].
IC50 & Target
Pyrrolobenzodiazepines
体外研究 (In Vitro)
SG3199 (HY-101161) is the released warhead component of the ADC payload Tesirine. SG3199 inhibits K562, NCIN87, BT474, and SKBR3 cancer cells with IC50s of 150 pM, 20 pM, 1 nM and 320 pM[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量
1496.65
Formula
C75H101N9O23
CAS 号
1595275-62-9
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°C, protect from light, stored under nitrogen
*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
溶解性数据
In Vitro:
DMSO : 200 mg/mL (133.63 mM; Need ultrasonic)
配制储备液
浓度溶剂体积质量
1 mg
5 mg
10 mg
1 mM
0.6682 mL
3.3408 mL
6.6816 mL
5 mM
0.1336 mL
0.6682 mL
1.3363 mL
10 mM
0.0668 mL
0.3341 mL
0.6682 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, stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
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]. Tiberghien AC, et al. Design and Synthesis of Tesirine, a Clinical Antibody-Drug Conjugate Pyrrolobenzodiazepine Dimer Payload. ACS Med Chem Lett. 2016;7(11):983-987. Published 2016 May 24.
[2]. Hartley JA, et al. Pre-clinical pharmacology and mechanism of action of SG3199, the pyrrolobenzodiazepine (PBD) dimer warhead component of antibody-drug conjugate (ADC) payload tesirine. Sci Rep. 2018;8(1):10479. Published 2018 Jul 11.
Nanocs provides a number of different sized silica particles coated with a thin layer of gold on their surface. Thickness of this gold layer ranges from 20-100 nm. These gold coated silica particles have high affinity toward proteins, antibodies, peptides and nucleic acids. With their high affinity to biomolecules, our gold coated silica particles can be used for biomolecule and cell detection, purification and separation.
Nanocs provides a number of different sized silica particles coated with a thin layer of gold on their surface. Thickness of this gold layer ranges from 20-100 nm. These gold coated silica particles have high affinity toward proteins, antibodies, peptides and nucleic acids. With their high affinity to biomolecules, our gold coated silica particles can be used for biomolecule and cell detection, purification and separation.
SG3199-Val-Ala-PAB is an intermediate of Tesirine synthesis. Tesirine is a drug-linker conjugate for ADC which can be used for the research of several cancers[1].
体外研究 (In Vitro)
SG3199-Val-Ala-PAB is an intermediate in in the synthesis of Tesirine, an antibody-drug conjugate pyrrolobenzodiazepine dimer payload[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
922.03
Formula
C49H59N7O11
CAS 号
1595275-61-8
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°C, protect from light, stored under nitrogen
*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
溶解性数据
In Vitro:
DMSO : 130 mg/mL (140.99 mM; Need ultrasonic)
配制储备液
浓度溶剂体积质量
1 mg
5 mg
10 mg
1 mM
1.0846 mL
5.4228 mL
10.8456 mL
5 mM
0.2169 mL
1.0846 mL
2.1691 mL
10 mM
0.1085 mL
0.5423 mL
1.0846 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, stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
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]. Tiberghien AC, et, al. Design and Synthesis of Tesirine, a Clinical Antibody-Drug Conjugate Pyrrolobenzodiazepine Dimer Payload. ACS Med Chem Lett. 2016 May 24;7(11):983-987.
