SJG-136
Based on 3 publication(s) in Google Scholar
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.
- Purity: 99.47%
- CAS No.: 232931-57-6
- Formula: C31H32N4O6
- Molecular Weight:556.61
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Protocol
- Purity & Documentation
- References
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) SJG-136
More
Biological Activity
|
Pyrrolobenzodiazepines |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CH1 | IC50 |
0.00012 μM
Compound: 5
|
Inhibition of cell growth in human ovarian carcinoma cell line (CH1) was determined using the 96 hour continuous exposure sulforhodamine B (SRB) growth delay assay.
Inhibition of cell growth in human ovarian carcinoma cell line (CH1) was determined using the 96 hour continuous exposure sulforhodamine B (SRB) growth delay assay.
|
[PMID: 11262084] |
| CH1 | IC50 |
0.12 nM
Compound: 5
|
Inhibition of cell growth in human ovarian carcinoma cell line (CH1) was determined using the 96 hour continuous exposure sulforhodamine B (SRB) growth delay assay.
Inhibition of cell growth in human ovarian carcinoma cell line (CH1) was determined using the 96 hour continuous exposure sulforhodamine B (SRB) growth delay assay.
|
[PMID: 11262084] |
| K562 | IC50 |
0.0425 μM
Compound: 5
|
Inhibition of cell growth by 50% in human leukemia cell line (K562) was determined using microculture tetrazolium (MTT) assay.
Inhibition of cell growth by 50% in human leukemia cell line (K562) was determined using microculture tetrazolium (MTT) assay.
|
[PMID: 11262084] |
| K562 | IC50 |
0.043 μM
Compound: 4a
|
Inhibitory concentration against human K562 leukemia cells following incubation for 1 hour
Inhibitory concentration against human K562 leukemia cells following incubation for 1 hour
|
[PMID: 14971896] |
| K562 | GI50 |
0.0038 μM
Compound: 4, SJG-136
|
Cytotoxicity against human K562 cell line after 96 hrs by MTT assay
Cytotoxicity against human K562 cell line after 96 hrs by MTT assay
|
[PMID: 16942018] |
| K562 | GI50 |
0.008 μM
Compound: 1
|
Cytotoxicity against human K562 cells
Cytotoxicity against human K562 cells
|
[PMID: 18272367] |
| K562 | GI50 |
0.419 nM
Compound: 6, SJG-136, SG2000
|
Cytotoxicity against human K562 cells by alamar blue assay
Cytotoxicity against human K562 cells by alamar blue assay
|
[PMID: 19811912] |
| Panel NCI-60 (60 carcinoma cell lines) | GI50 |
0.0074 μM
Compound: 4, SJG-136
|
Cytotoxicity against human NCI60 cell line by MTT assay
Cytotoxicity against human NCI60 cell line by MTT assay
|
[PMID: 16942018] |
| Panel NCI-60 cells | GI50 |
0.0074 μM
Compound: 4, SJG-136
|
Cytotoxicity against human NCI60 cell line by MTT assay
Cytotoxicity against human NCI60 cell line by MTT assay
|
[PMID: 16942018] |
| SK-OV-3 | IC50 |
0.0091 μM
Compound: 5
|
Inhibition of cell growth in human ovarian carcinoma cell line(SKOV-3) using the 96 hour continuous exposure sulforhodamine B (SRB) growth delay assay
Inhibition of cell growth in human ovarian carcinoma cell line(SKOV-3) using the 96 hour continuous exposure sulforhodamine B (SRB) growth delay assay
|
[PMID: 11262084] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 232931-57-6
-
Appearance Solid
-
Molecular Weight 556.61
-
Formula C31H32N4O6
-
Color White to yellow
-
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
-
Synonyms
NSC-694501
-
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
Publications (3)
-
Journal Impact Factor
-
Most Recent
Solvent & Solubility
DMSO : 33.33 mg/mL (59.88 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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
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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
-
Data Sheet (280 KB)
-
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
-
Handling Instructions (2659 KB)
References
[1]. Gregson SJ, et al. Design, synthesis, and evaluation of a novel pyrrolobenzodiazepine DNA-interactive agent with highly efficient cross-linking ability and potent cytotoxicity. J Med Chem. 2001 Mar 1;44(5):737-48. [Content Brief]
[2]. Mellinas-Gomez M, et al. Activity of the DNA minor groove cross-linking agent SG2000 (SJG-136) against canine tumours. BMC Vet Res. 2015 Aug 19;11:215. [Content Brief]
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. 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 | 1.7966 mL | 8.9830 mL | 17.9659 mL | 44.9148 mL |
| 5 mM | 0.3593 mL | 1.7966 mL | 3.5932 mL | 8.9830 mL | |
| 10 mM | 0.1797 mL | 0.8983 mL | 1.7966 mL | 4.4915 mL | |
| 15 mM | 0.1198 mL | 0.5989 mL | 1.1977 mL | 2.9943 mL | |
| 20 mM | 0.0898 mL | 0.4491 mL | 0.8983 mL | 2.2457 mL | |
| 25 mM | 0.0719 mL | 0.3593 mL | 0.7186 mL | 1.7966 mL | |
| 30 mM | 0.0599 mL | 0.2994 mL | 0.5989 mL | 1.4972 mL | |
| 40 mM | 0.0449 mL | 0.2246 mL | 0.4491 mL | 1.1229 mL | |
| 50 mM | 0.0359 mL | 0.1797 mL | 0.3593 mL | 0.8983 mL |
SJG-136 Related Classifications
HY-14573 Related Classifications
Powered by Bioz