| Field | Specification |
|---|---|
| Target | |
| Alternative names | 108600 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C22H14Cl2N2O6S2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
ON 108600, also known as 108600, is an inhibitor of CK2 (CK2α1 IC50 = 50 nM; CK2α2 IC50 = 5 nM), TNIK (IC50 = 5 nM), and DYRK family kinases (DYRK1A IC50 = 16 nM; DYRK1B IC50 = 7 nM; DYRK2 IC50 = 28 nM). It suppresses the growth of CD44high/CD24low breast cancer stem cell (BCSC) populations, induces G2/M arrest and apoptosis in triple-negative breast cancer (TNBC) cells, and inhibits tubulin polymerization, supporting its use in studying chemotherapy-resistant and metastatic TNBC[1][2]. It is supplied as a brown to reddish brown solid (C22H14Cl2N2O6S2, MW 537.39) at 98.65% purity.
Physical & Chemical Properties
| CAS Number | 1585246-23-6 |
|---|---|
| Molecular Formula | C22H14Cl2N2O6S2 |
| Molecular Weight | 537.39 g/mol |
| Purity | 98.65% |
| Appearance | Solid |
| Color | Brown to reddish brown |
| SMILES | ClC(C=CC=C1Cl)=C1CS(=O)(C2=CC=C(S/C(C(N3)=O)=C\C4=CC([N+]([O-])=O)=C(C=C4)O)C3=C2)=O |
| Target | DYRK2, DYRK1A, DYRK1B, CK2α2, CK2α1 |
| Signaling Pathway | Cell Cycle/DNA Damage; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt; Apoptosis; Cytoskeleton |
| Solubility | In Vitro: DMSO: 100 mg/mL (186.08 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[1]
|
DYRK2 0.028 μM (IC50) |
DYRK1A 0.016 μM (IC50) |
DYRK1B 0.007 μM (IC50) |
CK2α2 0.005 μM (IC50) |
CK2α1 0.05 μM (IC50) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
[2]. Özkan A D, et al. Determination of the Apoptotic Effect of Raf2 and Nck-Interacting Protein Kinase Inhibitor on Metastatic Canine Mammary Gland Tumor Cells[J]. Online Turkish Journal of Health Sciences, 7(1): 117-122.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 100 mg/mL (186.08 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); avoid repeated freeze-thaw cycles.
Data provided by the manufacturer.
In Vitro
In the TNBC cell lines MDA-MB-231, MDA-MB-468, Hs578T and BT-20, ON 108600 (108600) (24-72 h) reduces viability with GI50 values of 0.1-0.2 μM, while showing little or no toxicity toward normal cells, such as MCF-10A, NBSC-1, NBSC-2, PBMC, HFL and hMSC-TERT (GI50 > 2.5 μM)[1]. In MDA-MB-231 and Hs578T cells, ON 108600 (0.1-3 μM; 24 h) blocks phosphorylation of the CK2α substrate AKT1 (Ser129), the DYRK1A substrates CYCLIN D1 (Thr286) and p27 (Ser10), and the TNIK substrate AXIN2[1]. ON 108600 (10-1000 nM; 72 h) suppresses the formation of colonies and mammospheres by CD44high/CD24low BCSC populations that were purified from MDA-MB-231 and Hs578T cells[1]. ON 108600 inhibits the recombinant kinases CK2α1, CK2α2, TNIK, DYRK1A, DYRK1B and DYRK2[1]. ON 108600 (72 h) triggers G2/M arrest and apoptosis in MDA-MB-231 cells and CTG1883 TNBC organoids[1]. In HeLa cells, ON 108600 (1 μM; 12 h) causes abnormal mitotic spindle formation, with multipolar spindles and multiple centrosomes[1]. ON 108600 (72 h) suppresses growth and colony formation in MDA-MB-231 and BT-20 cells resistant to Paclitaxel (MDA-MB-231-TR and BT-20-TR) just as efficiently as in the parental paclitaxel-sensitive cells[1]. In metastatic canine mammary gland tumor (CMGT) cells, ON 108600 (2.5 and 5 μM; 48 h) decreases cell viability and induces G0/G1 arrest and apoptosis[2].
Cell Proliferation Assay[1]
| Cell Line | MDA-MB-231 (CD44high/CD24low), Hs578T (CD44high/CD24low) |
|---|---|
| Concentration | 10, 100, 250, 500, 1000 nM |
| Incubation Time | 72 h |
| Result | Suppressed colony formation in a dose-dependent manner. Suppressed mammosphere formation in a dose-dependent manner. |
Western Blot Analysis[1]
| Cell Line | MDA-MB-231, Hs578T |
|---|---|
| Concentration | 0.1, 0.5, 1.0, 1.5, 3.0 μM |
| Incubation Time | 24 h |
| Result | Inhibited phosphorylation of AKT1 (Ser129), CYCLIN D1 (Thr286) and p27 (Ser10). Reduced AXIN2 expression in a dose-dependent manner. |
Cell Cycle Analysis[1]
| Cell Line | MDA-MB-231, CTG1883 organoids |
|---|---|
| Concentration | 0.125, 0.25, 0.5 μM |
| Incubation Time | 24, 48, 72 h |
| Result | Induced G2/M arrest and increased sub-G1 fraction. |
Apoptosis Analysis[1]
| Cell Line | MDA-MB-231, CTG1883 organoids |
|---|---|
| Concentration | 0.25, 0.5, 1.0, 1.5, 3.0 μM |
| Incubation Time | 24,48 h |
| Result | Induced PARP and Caspase 3 cleavage in a dose-dependent manner. |
Immunofluorescence[1]
| Cell Line | HeLa |
|---|---|
| Concentration | 1 μM |
| Incubation Time | 12 h |
| Result | Induced abnormal mitotic spindle formation with multipolar spindles and multiple centrosomes. |
Cell Viability Assay[2]
| Cell Line | Canine mammary gland tumor (CMGT) cells |
|---|---|
| Concentration | 1, 2, 2.5, 3, 4, 5 μM |
| Incubation Time | 24, 48 h |
| Result | Inhibited cell viability in a dose- and time-dependent manner, with approximately 50% reduction at 2.5-5 μM for 48 h. |
Apoptosis Analysis[2]
| Cell Line | Canine mammary gland tumor (CMGT) cells |
|---|---|
| Concentration | 2.5, 5 μM |
| Incubation Time | 48 h |
| Result | Increased late apoptotic cells from 2.65% to 29.65% and 48.50%, respectively. |
Cell Cycle Analysis[2]
| Cell Line | Canine mammary gland tumor (CMGT) cells |
|---|---|
| Concentration | 2.5, 5 μM |
| Incubation Time | 48 h |
| Result | Induced G0/G1 arrest and increased G0/G1 population from 61.6% to 65.2% and 73.7%, respectively. |
Immunofluorescence[2]
| Cell Line | Canine mammary gland tumor (CMGT) cells |
|---|---|
| Concentration | 2.5, 5 μM |
| Incubation Time | 48 h |
| Result | Induced nuclear damage. |
In Vivo
In CTG1883 PDX tumor grafts in NSG mice, treatment with ON 108600 (108600) (100 mg/kg; i.p.; every other day for 5 days) blocks phosphorylation of CK2α and DYRK1A substrates (pAKT1 Ser129, pCYCLIN D1 Thr286) and lowers C-MYC expression[1]. ON 108600 (50 or 100 mg/kg; i.p.; every other day for 21 days) reduces tumor growth in the MDA-MB-231 xenograft model in nude mice, with no observable toxicity[1]. In the TM00098 model (Paclitaxel-sensitive TNBC PDX) in NSG mice, ON 108600 (100 mg/kg; i.p.; every other day for 21 days) curbs tumor growth with no adverse effects on body weight[1]. Combined with Paclitaxel, ON 108600 (100 mg/kg; i.p.; every other day for 12-24 days) synergistically curbs tumor growth in the chemotherapy-resistant TNBC PDX models CTG1883 and CTG2397[1]. In the MDA-MB-231/LM2-4/mCherry metastatic model in NSG mice, the growth of lung metastases that were already established is curbed by ON 108600 (100 mg/kg; i.p.; every other day for 14 days) combined with Paclitaxel[1].
| Animal Model | CTG1883 PDX tumor-bearing female NSG mice (8-12 weeks old)[1] |
|---|---|
| Dosage | 100 mg/kg |
| Administration | i.p.; every other day for 5 days |
| Result | Inhibited phosphorylation of pAKT1 Ser129 and pCYCLIN D1 Thr286. Reduced C-MYC expression in tumors. |
| Animal Model | MDA-MB-231 xenograft-bearing female athymic nude mice (8-12 weeks old)[1] |
|---|---|
| Dosage | 50, 100 mg/kg |
| Administration | i.p.; every other day for 21 days |
| Result | Inhibited tumor growth in a dose-dependent manner, with no observable toxicity or body weight loss. |
| Animal Model | TM00098 PDX tumor-bearing female NSG mice (8-12 weeks old)[1] |
|---|---|
| Dosage | 100 mg/kg |
| Administration | i.p.; every other day for 21 days |
| Result | Suppressed tumor growth without adverse effects on body weight. |
| Animal Model | CTG1883 and CTG2397 PDX tumor-bearing female NSG mice (8-12 weeks old)[1] |
|---|---|
| Dosage | 100 mg/kg |
| Administration | i.p.; every other day for 12-24 days |
| Result | Suppressed tumor growth. |
| Animal Model | MDA-MB-231/LM2-4/mCherry metastatic model (lung metastases) in female NSG mice (7 weeks old)[1] |
|---|---|
| Dosage | 100 mg/kg |
| Administration | i.p.; every other day for 14 days |
| Result | Suppressed growth of pre-established lung metastases. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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