2. Cell Cycle/DNA Damage Antibody-drug Conjugate/ADC Related
  3. DNA Alkylator/Crosslinker ADC Cytotoxin
  4. SG2057

SG2057 (DRG16) is a PBD dimer containing a pentyldioxy linkage which binds sequence selectively in the minor groove of DNA forming DNA interstrand and intrastrand cross-linked adducts. SG2057 is a highly active antitumor agent.

For research use only. We do not sell to patients.

SG2057 Chemical Structure

SG2057 Chemical Structure

CAS No. : 260417-62-7

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1 mg USD 285 In-stock
5 mg USD 850 In-stock
10 mg USD 1450 In-stock
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Based on 1 publication(s) in Google Scholar

SG2057 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

SG2057 (DRG16) is a PBD dimer containing a pentyldioxy linkage which binds sequence selectively in the minor groove of DNA forming DNA interstrand and intrastrand cross-linked adducts. SG2057 is a highly active antitumor agent[1].

IC50 & Target[1]

Pyrrolobenzodiazepines

 

In Vitro

SG2057 has multilog differential in vitro cytotoxicity against a panel of human tumour cell lines with a mean GI50 of 212 pM. SG2057 is highly efficient at producing DNA interstrand cross-links in cells which form rapidly and persist over a 48 h period[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SG2057 Related Antibodies
In Vivo

SG2057 (5-60 μg/kg; i.v) exhibits dose-dependent antitumor activity in human tumor xenograft models[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female NCr-nude mice injected with SKOV-3 cells[1]
Dosage: 5 μg/kg, 10 μg/kg, 20 μg/kg, 30 μg/kg, 40 μg/kg, 50 μg/kg, 60 μg/kg
Administration: i.v.; daily, once a week, or once every four days
Result: Showed significant antitumor activity.
Molecular Weight

584.66

Formula

C33H36N4O6
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C1N2[C@](CC(C2)=C)([H])C=NC3=CC(OCCCCCOC4=C(OC)C=C5C(N6[C@](CC(C6)=C)([H])C=NC5=C4)=O)=C(OC)C=C13
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, stored under nitrogen

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

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (171.04 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.28 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.28 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 97.31% ee.: 100.00%

COA (249 KB) HNMR (456 KB) NP-HPLC (101 KB) LCMS (100 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7104 mL 8.5520 mL 17.1040 mL 42.7599 mL
5 mM 0.3421 mL 1.7104 mL 3.4208 mL 8.5520 mL
10 mM 0.1710 mL 0.8552 mL 1.7104 mL 4.2760 mL
15 mM 0.1140 mL 0.5701 mL 1.1403 mL 2.8507 mL
20 mM 0.0855 mL 0.4276 mL 0.8552 mL 2.1380 mL
25 mM 0.0684 mL 0.3421 mL 0.6842 mL 1.7104 mL
30 mM 0.0570 mL 0.2851 mL 0.5701 mL 1.4253 mL
40 mM 0.0428 mL 0.2138 mL 0.4276 mL 1.0690 mL
50 mM 0.0342 mL 0.1710 mL 0.3421 mL 0.8552 mL
60 mM 0.0285 mL 0.1425 mL 0.2851 mL 0.7127 mL
80 mM 0.0214 mL 0.1069 mL 0.2138 mL 0.5345 mL
100 mM 0.0171 mL 0.0855 mL 0.1710 mL 0.4276 mL
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SG2057 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SG2057260417-62-7DRG16SG 2057SG-2057DRG 16DRG-16DNA Alkylator/CrosslinkerADC CytotoxinADC Payloadantitumor activityPBD dimerpentyldioxy linkageInhibitorinhibitorinhibit

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