1. Cell Cycle/DNA Damage Antibody-drug Conjugate/ADC Related
  2. DNA Alkylator/Crosslinker ADC Cytotoxin
  3. SJG-136

SJG-136  (Synonyms: NSC-694501)

Cat. No.: HY-14573 Purity: 99.43%
COA Handling Instructions

SJG-136 is a DNA cross-linking agent, with an XL50 of 45 nM for pBR322 DNA. SJG-136 has potent antitumor activity.

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

SJG-136 Chemical Structure

SJG-136 Chemical Structure

CAS No. : 232931-57-6

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 527 In-stock
Solution
10 mM * 1 mL in DMSO USD 527 In-stock
Solid
1 mg USD 280 In-stock
5 mg USD 430 In-stock
10 mg USD 690 In-stock
25 mg USD 1380 In-stock
50 mg USD 2200 In-stock
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE SJG-136

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

SJG-136 is a DNA cross-linking agent, with an XL50 of 45 nM for pBR322 DNA. SJG-136 has potent antitumor activity.

IC50 & Target[1]

Pyrrolobenzodiazepines

 

In Vitro

SJG-136 (dimer 5) is a DNA cross-linking agent, with an XL50 (concentration of agent required for 50% cross-linking of pBR322 DNA) of 45 nM for pBR322 DNA. SJG-136 is cytotoxic to ovarian cell lines, such as A2780 (IC50, 22.5 pM), A2780cisR (IC50, 24 pM), CH1 (IC50, 0.12 nM), CH1cisR (IC50, 0.6 nM), and SKOV-3 (IC50, 9.1 nM)[1]. SJG-136 (SG2000) also reduces the viability of a panel of canine cancer cells, with GI50 values ranging from 0.33 - >100 nM after a 1 h exposure, and <0.03 - 17.33 nM following continuous exposure[2].

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

In Vivo

SJG-136 shows more potent antitumor effect against CMeC-1 tumour at 0.30 mg/kg than 0.15 mg/kg either as a single dose or administered once a week for three weeks via dosed intravenously in mice. SJG-136-induced H2AX phosphorylation shows good correspondence, but less sensitivity, than measurement of foci[2].

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

Clinical Trial
Molecular Weight

556.61

Appearance

Solid

Formula

C31H32N4O6

CAS No.
SMILES

O=C1N2[C@@H](CC(C2)=C)C=NC3=CC(OCCCOC4=C(OC)C=C(C(N(CC(C5)=C)[C@@H]5C=N6)=O)C6=C4)=C(OC)C=C31

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (59.88 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7966 mL 8.9830 mL 17.9659 mL
5 mM 0.3593 mL 1.7966 mL 3.5932 mL
10 mM 0.1797 mL 0.8983 mL 1.7966 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (4.49 mM); Clear solution

  • 2.

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

    Solubility: 2.08 mg/mL (3.74 mM); Suspended solution; Need ultrasonic

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (3.74 mM); Clear solution

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 99.43%

References
Cell Assay
[1]

In vitro cytotoxicity is evaluated using the human ovarian carcinoma cell lines SKOV-3, A2780, and CH1, together with the cisplatin-resistant counterparts of the A2780 and CH1 lines (A2780cisR and CH1cisR, respectively). Viable cells are seeded in growth medium (160 μL) into 96-well microtiter plates and allowed to attach overnight. SJG-136 is dissolved in DMSO (to give a 20 mM concentration in each case) immediately prior to adding to the cells in quadruplicate wells. Final drug concentrations in the wells ranged from 100 μM to 2.5 nM as follows: 100, 25, 10, 2.5, 1 μM, and 250, 100, 25, 10, 2.5 nM. This is achieved by diluting the drugs in growth medium and then adding 40 μL to the existing well volume of 160 μL to give the final concentrations stated above. After 4 days (96 h), the medium is removed and the remaining cells are fixed using 10% trichloroacetic acid on ice for 30 min. Wells are then washed 3−4 times with tap water and air-dried overnight, and 100 μL of 0.4% sulforhodamine B (dissolved in 1% glacial HOAc) is added to each well. Staining is allowed to continue for 10−15 min; the wells are then washed 3−4 times with 1% acetic acid and air-dried, and Tris base (100 μL of 10 mM) is added to each one. The plates are then shaken and absorbance readings taken at 540 nm using a plate reader. From plots of concentration versus percentage absorbance (compared to 8 untreated wells), IC50 values are calculated using the Quattro-Pro software package[1].

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

Animal Administration
[2]

A homogenous suspension of 5 × 106 exponentially growing canine melanoma cells in serum free RPMI 1640 tissue culture medium is injected subcutaneously into CD1 Nu/Nu immunocompromised female mice. The mice are divided into five groups of ten mice, with equivalent mean tumour volumes for each group. SJG-136 is given intravenously into the tail vein to four of these groups and vehicle control is administered to the fifth group. SJG-136 injections are prepared in 0.9 % NaCl and 1 % DMSO vehicle. Animals are weighed prior to the injection to determine the volume of SJG-136 required (0.1 mL/10 g body weight) which is given IV in the tail vein. Control group mice are given an IV injection of the vehicle solution; mice in groups one and two are given a single treatment of SJG-136, 0.15 mg/kg and 0.30 mg/kg respectively; mice in groups four and five are given 0.15 mg/kg and 0.30 mg/kg respectively, every seven days for a total of three treatments[2].

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

References
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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.

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Product Name:
SJG-136
Cat. No.:
HY-14573
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