2. Cell Cycle/DNA Damage Antibody-drug Conjugate/ADC Related
  3. DNA Alkylator/Crosslinker ADC Cytotoxin
  4. SG3199

SG3199 is a cytotoxic DNA minor groove interstrand crosslinking pyrrolobenzodiazepine (PBD) dimer. SG3199 is the released warhead component of the ADC payload Tesirine (SG3249).

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

SG3199 Chemical Structure

SG3199 Chemical Structure

CAS No. : 1595275-71-0

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1 mg USD 850 In-stock
5 mg USD 2500 In-stock
10 mg USD 3750 In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

SG3199 Related Antibodies

Top Publications Citing Use of Products
Cell Viability Assay

    SG3199 purchased from MedChemExpress. Usage Cited in: Mol Pharm. 2022 Dec 2.  [Abstract]

    Both DM1 and SG3199 (0.1-200 μM; 5 min) inhibits SLC46A3 dC-mediated 5-CF (1 μM) uptake in a concentration-dependent manner, with the IC50s of 16.4 and 43.6 μM, respectively, in MDCKII/SLC46A3 dC cells.

    View All ADC Cytotoxin Isoform Specific Products:

    View All Isoforms
    Auristatin Calicheamicins Camptothecins Daunorubicins/Doxorubicins Duocarmycins Maytansinoids Pyrrolobenzodiazepines Traditional Cytotoxic Agents

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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

     

    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].

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

    SG3199 Related Antibodies
    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].

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

    584.66

    Formula

    C33H36N4O6
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    Storage

    -20°C, protect from light, stored under nitrogen

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

    Solvent & Solubility
    In Vitro: 

    DMSO : 130 mg/mL (222.35 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 (protect from light, 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
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    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: ≥ 3.25 mg/mL (5.56 mM); Clear solution

      This protocol yields a clear solution of ≥ 3.25 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (32.5 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: ≥ 3.25 mg/mL (5.56 mM); Clear solution

      This protocol yields a clear solution of ≥ 3.25 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 (32.5 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 (protect from light, 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: 98.94%

    COA (248 KB) HNMR (265 KB) RP-HPLC (204 KB) LCMS (109 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 (protect from light, 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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    SG3199 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:

    SG31991595275-71-0SG 3199SG-3199DNA Alkylator/CrosslinkerADC CytotoxinADC PayloadcytotoxicitypyrrolobenzodiazepinePBDdimerDNAcross-linkingADCInhibitorinhibitorinhibit

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