2. JAK/STAT Signaling Stem Cell/Wnt Apoptosis
  3. STAT Apoptosis
  4. Danvatirsen

Danvatirsen (AZD9150) is an antisense oligonucleotide targeting STAT3. Danvatirsen reduces the viability and promotes apoptosis of leukemia cell lines. Danvatirsen inhibits the expression of endogenous STAT3 and its downstream target genes, and reduces the proliferation and tumorigenicity of neuroblastoma and lymphoma cells. Danvatirsen inhibited tumor growth in mouse models of neuroblastoma, lymphoma, and non-small cell lung cancer. Danvatirsen achieves STAT3 mRNA and protein depletion in a mouse model of epidermoid carcinoma. Danvatirsen can be used in research related to lymphoma, myelodysplastic syndrome, acute myeloid leukemia, neuroblastoma and non-small cell lung cancer.

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

DNA, d(P-thio)([(5′ξ)-2′,5′-anhydro-6′-deoxy-4′-C-(hydroxymethyl)-α-L-lyxo-hexofurano]m5C-(3′→4′)-[(5′ξ)-2′,5′-anhydro-6′-deoxy-4′-C-(hydroxymethyl)-α-L-lyxo-hexofurano]m5U-(3′→4′)-[(5′ξ)-2′,5′-anhydro-6′-deoxy-4′-C-(hydroxymethyl)-α-L-lyxo-hexofurano]A-T-T-T-G-G-A-T-G-T-m5C-(3′→4′)-[(5′ξ)-2′,5′-anhydro-6′-deoxy-4′-C-(hydroxymethyl)-α-L-lyxo-hexofurano]A-(3′→4′)-[(5′ξ)-2′,5′-anhydro-6′-deoxy-4′-C-(hydroxymethyl)-α-L-lyxo-hexofurano]G-(3′→4′)-[(5′ξ)-2′,5′-anhydro-6′-deoxy-4′-C-(hydroxymethyl)-α-L-lyxo-hexofurano]m5C)

Danvatirsen Chemical Structure

CAS No. : 1402357-06-5

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Description

Danvatirsen (AZD9150) is an antisense oligonucleotide targeting STAT3. Danvatirsen reduces the viability and promotes apoptosis of leukemia cell lines. Danvatirsen inhibits the expression of endogenous STAT3 and its downstream target genes, and reduces the proliferation and tumorigenicity of neuroblastoma and lymphoma cells. Danvatirsen inhibited tumor growth in mouse models of neuroblastoma, lymphoma, and non-small cell lung cancer. Danvatirsen achieves STAT3 mRNA and protein depletion in a mouse model of epidermoid carcinoma. Danvatirsen can be used in research related to lymphoma, myelodysplastic syndrome, acute myeloid leukemia, neuroblastoma and non-small cell lung cancer[1][2][3][4].

In Vitro

Danvatirsen (2.5-10 μM) significantly reduces STAT3 mRNA levels in KG1a, CMK, MOLM13 and KT1 leukemia cell lines[2].
Danvatirsen (1-10 μM; 24-72 h) significantly reduces the viability of leukemia/myelodysplastic syndrome (MDS) cell lines including NB4, MOLM14, MDS-L, MV411, KG1a, MOLM13, KT1 and CMK[2].
Danvatirsen (5 μM for CMK, 10 μM for KT1 and U937; 48 h) significantly increases the apoptosis levels of CMK, KT1 and U937 leukemia cell lines[2].
Danvatirsen (2.5-10 μM; 24 h) significantly reduces STAT3 mRNA levels in primary MDS/AML stem cells[2].
Danvatirsen (10 μM; 14 days) enhances erythroid and myeloid differentiation of primary myelodysplastic syndrome (MDS) stem/progenitor cells[2].
Danvatirsen (10 μM; 24 h) downregulates STAT3 and its downstream oncogenic target genes (IL1RAP, MSI2, MCL1, IL8, CXCR2) at the mRNA level, and reduces the protein levels of STAT3, phosphorylated STAT3 and MCL1 in CMK leukemia cells[2].
Danvatirsen induces dose-dependent apoptosis in primary TP53-mutant MDS/AML stem/progenitor cells and reduces the replating efficiency of primary AML stem and progenitor cells in colony-forming assays[2].
Danvatirsen (0.25-10 μM; 6 days) dose-dependently inhibits STAT3 mRNA expression in SK-N-AS, NGP and IMR32 neuroblastoma cells, with IC50 values of 0.69, 0.64 and 0.76 μM, respectively[3].
Danvatirsen (0.25-10 μM; 6 days) dose-dependently inhibits the expression of total STAT3 protein and phosphorylated STAT3 protein in SK-N-AS, NGP and IMR32 neuroblastoma cells, with IC50 values of 0.99 μM, 0.97 μM and 0.98 μM, respectively[3].
Danvatirsen (1 μM; 6 days) significantly reduces the mRNA and protein expression levels of multiple STAT3 target genes in SK-N-AS, NGP and IMR32 neuroblastoma cells[3].
Danvatirsen (1 μM; 4 weeks) significantly inhibits the proliferation of SK-N-AS, NGP and IMR32 neuroblastoma cells, reducing the maximum cell confluence by up to 38%, 37% and 34% respectively during continuous incubation. It also suppresses the anchorage-independent colony formation of the cells, decreasing the number of colonies by 20%, 43% and 67% respectively[3].
Danvatirsen (1 μM; 6 days) significantly enhances the sensitivity of SK-N-AS, NGP and IMR32 neuroblastoma cells to Cisplatin (HY-17394), reduces the IC50 value of Cisplatin by up to 2-fold, and attenuates the activation of Cisplatin-induced DNA damage response pathways[3].
Danvatirsen (0.005-5 μM; 5 days) dose-dependently inhibits the proliferation of STAT3-dependent human lymphoma cell lines KARPAS299 and SUP-M2 via free uptake[4].

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

Danvatirsen Related Antibodies

Cell Viability Assay[2]

Cell Line: NB4, MOLM14, MDS-L, MV411, KG1a, MOLM13, KT1, CMK leukemic/MDS cell lines
Concentration: 10 μM
Incubation Time: 24 h, 48 h, 72 h
Result: Induced a significant, dose-dependent decrease in cell viability across all tested cell lines.
Showed greater inhibition at higher concentrations.

Apoptosis Analysis[2]

Cell Line: CMK, KT1, U937 leukemic cell lines
Concentration: 5 μM (CMK cells); 10 μM (KT1 and U937 cells)
Incubation Time: 48 h
Result: Induced a significant increase in early apoptotic, late apoptotic, and necrotic cell populations compared with controls.
Showed a dose-dependent effect observed across tested concentrations.

Real Time qPCR[2]

Cell Line: CMK leukemic cells
Concentration: 10 μM
Incubation Time: 24 h
Result: Downregulated expression of STAT3 and oncogenic/stem cell-associated genes including IL1RAP, MSI2, MCL1, IL8, and CXCR2 at the mRNA level.

Western Blot Analysis[2]

Cell Line: CMK leukemic cells
Concentration: 10 μM
Incubation Time: 24 h
Result: Reduced STAT3 protein, phospho-STAT3, and MCL1 protein levels.

Real Time qPCR[3]

Cell Line: SK-N-AS, NGP, IMR32 human neuroblastoma cell lines
Concentration: 0.25-10 μM
Incubation Time: 6 days
Result: Inhibited STAT3 mRNA levels in a dose-dependent manner.
Achieved IC50 values of 0.69 μM in SK-N-AS cells, 0.64 μM in NGP cells, and 0.76 μM in IMR32 cells.

Western Blot Analysis[3]

Cell Line: SK-N-AS, NGP, IMR32 human neuroblastoma cell lines
Concentration: 0.25-10 μM
Incubation Time: 6 days
Result: Decreased both total and phosphorylated STAT3 (Ser727, Tyr705) protein levels in a dose-dependent manner.
Achieved IC50 values of 0.99 μM in SK-N-AS cells, 0.97 μM in NGP cells, and 0.98 μM in IMR32 cells.

Cell Proliferation Assay[3]

Cell Line: SK-N-AS, NGP, IMR32 human neuroblastoma cell lines
Concentration: 1 μM
Incubation Time: continuous incubation (up to 240 hours)
Result: Caused a significant decrease in cell growth: up to 38% decrease in SK-N-AS cells, up to 37% decrease in NGP cells, and up to 34% decrease in IMR32 cells.

Cell Viability Assay[3]

Cell Line: SK-N-AS, NGP, IMR32 human neuroblastoma cell lines
Concentration: 1 μM
Incubation Time: 3 days pre-incubation, followed by 3 days co-incubation with cisplatin
Result: Significantly increased cisplatin sensitivity, resulting in a 2-fold decrease in cisplatin IC50 in NGP cells and IMR32 cells, and a smaller decrease in SK-N-AS cells.
Attenuated cisplatin-induced activation of the ATM and ATR DNA damage response pathways, as shown by reduced phosphorylation of ATM, Chk2, ATR, Chk1, and γH2AX.

Cell Proliferation Assay[4]

Cell Line: KARPAS299, SUP-M2 (human lymphoma cell lines)
Concentration: 0.005-5 μM
Incubation Time: 5 days
Result: Induced dose-dependent inhibition of cell proliferation in KARPAS299 and SUP-M2 cells.
Showed antiproliferative effects that correlated with the degree of STAT3 depletion.
In Vivo

Danvatirsen (50 mg/kg, s.c., 5 days per week for 4 consecutive weeks) significantly reduces the engraftment rate of human MDS/AML cells in NSG mice[2].
Combination of Danvatirsen (100 mg/kg; s.c.; 5 times per week for 3 consecutive weeks) with Cisplatin results in a maximum growth inhibition rate of 38% in neuroblastoma xenografts and significantly prolongs the survival of tumor-bearing mice[3].
Danvatirsen (25-50 mg/kg; s.c.; 5 times per week; for 3 consecutive weeks) induces potent, dose-dependent depletion of STAT3 mRNA and protein in human epidermoid carcinoma A431 xenografts, with the 25 mg/kg dose reducing tumor STAT3 mRNA levels by 90%[4].
Danvatirsen (50 mg/kg, s.c., 5 times per week for 5 weeks) inhibits the growth of human lymphoma SUP-M2 xenografts with an inhibition rate of 62%, and reduces tumor STAT3 mRNA levels by approximately 40%. It exhibits systemic anti-lymphoma activity in the disseminated SUP-M2 model, reducing tumor STAT3 mRNA by approximately 50% and decreasing plasma concentrations of sIL-2Rα and sCD30[4].
Danvatirsen (25 mg/kg; s.c.; 5 times per week; for approximately 5 weeks) inhibits the growth of PC-9 human non-small cell lung cancer xenografts by 90%, and reduces STAT3 activity and the expression of its downstream target genes[4].

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

Animal Model: Nonobese Diabetic Scid Gamma (NSG) (irradiated, engrafted with primary human MDS/AML peripheral blood mononuclear cells)[2]
Dosage: 50 mg/kg
Administration: s.c.; 5 days per week; 4 weeks
Result: Reduced MDS/AML burden, with greatly decreased fold change of human CD45+ cells in bone marrow compared with controls.
Achieved complete loss of detectable human CD45+ cells in some treated mice.
Exerted effects in both low-risk and high-risk MDS patient-derived xenografts.
Animal Model: athymic nude mice (5-6 week-old female)[3]
Dosage: 100 mg/kg (target reagent); 2 mg/kg (Cisplatin)
Administration: subcutaneous (target reagent; 5 times per week; 3 weeks); intraperitoneal (cisplatin; 2 times per week; 3 weeks; co-administered starting on day 11 of target reagent treatment)
Result: Reduced neuroblastoma xenograft growth by up to 38% compared to control-treated mice.
Prolonged survival significantly compared to control-treated mice.
Animal Model: Immunocompromised mice; NSG mice (disseminated lymphoma model)[4]
Dosage: 25 mg/kg; 37.5 mg/kg; 50 mg/kg
Administration: 5 times per week; 3 weeks (25 mg/kg, 50 mg/kg)
Result: Reduced tumor STAT3 mRNA by approximately 90% (P=0.0001) and STAT3 protein by 93% (25 mg/kg).
Produced near-complete depletion of STAT3 protein throughout the tumor as measured by immunohistochemistry (50 mg/kg).
Animal Model: NSG mice, Immunocompromised mice[4]
Dosage: 50 mg/kg
Administration: 5 times per week; 2, 5 weeks
Result: Reduced STAT3 mRNA by ~50% in tumors isolated from axillary lymph nodes and peritoneal cavity vs control groups.
Reduced plasma sIL-2Rα and sCD30 concentrations.
Reduced tumor burden (and ascites formation.
Achieved 67% tumor growth inhibition (TGI).
Confirmed inhibition of human STAT3 in tumor cells and murine STAT3 in tumor-associated stromal cells via species-specific PCR.
Confirmed reduced phospho-STAT3 protein in both human tumor and mouse stromal cells via immunohistochemistry.
No associated change in body weight was observed.
Animal Model: Immunocompromised mice[4]
Dosage: 25 mg/kg
Administration: 5 times per week; ~5 weeks
Result: Achieved 90% tumor growth inhibition (TGI) vs control .
Reduced tumor STAT3 and phospho-STAT3 protein, and reduced expression of STAT3 target genes c-MYC, MCL-1, and VEGF.
Molecular Weight

5422.00

CAS No.
Appearance

Solid

Color

White to off-white

Sequence

DNA, d(P-thio)([(5′ξ)-2′,5′-anhydro-6′-deoxy-4′-C-(hydroxymethyl)-α-L-lyxo-hexofurano]m5C-(3′→4′)-[(5′ξ)-2′,5′-anhydro-6′-deoxy-4′-C-(hydroxymethyl)-α-L-lyxo-hexofurano]m5U-(3′→4′)-[(5′ξ)-2′,5′-anhydro-6′-deoxy-4′-C-(hydroxymethyl)-α-L-lyxo-hexofurano]A-T-T-T-G-G-A-T-G-T-m5C-(3′→4′)-[(5′ξ)-2′,5′-anhydro-6′-deoxy-4′-C-(hydroxymethyl)-α-L-lyxo-hexofurano]A-(3′→4′)-[(5′ξ)-2′,5′-anhydro-6′-deoxy-4′-C-(hydroxymethyl)-α-L-lyxo-hexofurano]G-(3′→4′)-[(5′ξ)-2′,5′-anhydro-6′-deoxy-4′-C-(hydroxymethyl)-α-L-lyxo-hexofurano]m5C)
SMILES

[Danvatirsen]
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: 

H2O : 100 mg/mL (18.44 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.1844 mL 0.9222 mL 1.8443 mL
5 mM 0.0369 mL 0.1844 mL 0.3689 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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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

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In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 50 mg/mL (9.22 mM); Clear solution; Need ultrasonic

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

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: 99.12%

SDS (252 KB)

COA (248 KB) LCMS (318 KB)

Handling Instructions (2242 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
H2O 1 mM 0.1844 mL 0.9222 mL 1.8443 mL 4.6108 mL
5 mM 0.0369 mL 0.1844 mL 0.3689 mL 0.9222 mL
10 mM 0.0184 mL 0.0922 mL 0.1844 mL 0.4611 mL
15 mM 0.0123 mL 0.0615 mL 0.1230 mL 0.3074 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • 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:

Danvatirsen1402357-06-5AZD9150AZD 9150AZD-9150STATApoptosisSTAT3 InhibitorMOLM14 cellsMDS-L cellsMV411 cellsKG1a cellsMOLM13 cellsKT1 cellsCMK leukemic/MDS cell linesSK-N-AS cellsNGP cellsIMR32 cellslymphomamyelodysplastic syndromeacute myeloid leukemianeuroblastoma and non-small cell lung cancerInhibitorinhibitorinhibit

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