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Fig. 1 · Structure
Cat. No.
A10244
CAS No.
35825-57-1
Formula
C19H20O3
Mol. Weight
296.4

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Cryptotanshinone

Cat. No. A10244 CAS 35825-57-1

Stat3 inhibitor

Cryptotanshinone, a natural compound isolated from the roots of Salvia miltiorrhiza Bunge (Danshen), dramatically blocks STAT3 Tyr705 phosphorylation but not STAT3 Ser727 phosphorylation in DU145 cells, and significantly inhibits JAK2 phosphorylation with IC50 of ~5 μM without affecting the phosphorylation of upstream kinases c-Src and EGFR.

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Biological Activity

Bioactivity / Mechanism

In U251 glioma cells, cryptotanshinone reduced STAT3 Tyr705 phosphorylation and increased SHP-2-associated phosphatase activity. NSC-87877 counteracted these effects, supporting phosphatase involvement in this model. These cellular assays do not establish direct binding to STAT3 or SHP-2. [1]

Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.

Target & Activity

Target Activity Value
STAT3 (HCT-116 cells) 4.6 μM

Cellular Effect

Cell Line Activity Value Description Reference
AGS IC50 1.58 μM Inhibition of HIF1 activation in human AGS cells assessed as inhibition of hypoxia-induced luciferase expression after 16 hrs by reporter assay [PMID: 17583950]
AGS IC50 10.2 μM Viability of human AGS cells under hypoxic conditions after 24 hrs by MTT assay [PMID: 17583950]
AGS IC50 13.5 μM Viability of human AGS cells under normoxic conditions after 24 hrs by MTT assay [PMID: 17583950]
BaF3 IC50 17.22 μM Growth inhibition of IL3-stimulated mouse BA/F3 cells after 48 hrs by CellTiter 96 assay [PMID: 23957426]
ECa-109 cell line IC50 5.01 μM Antitumor activity against human EC109 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay [PMID: 35504209]
HCT-116 IC50 4.6 μM Inhibition of STAT3 expressed in human HCT116 cells after 24 hrs by luciferase reporter gene assay [PMID: 22650325]
Hep 3B2 IC50 > 30 μM Viability of human Hep3B cells under normoxic conditions after 24 hrs by MTT assay [PMID: 17583950]
Hep 3B2 IC50 > 30 μM Viability of human Hep3B cells under hypoxic conditions after 24 hrs by MTT assay [PMID: 17583950]
Hep 3B2 IC50 1.36 μM Inhibition of HIF1 activation in human Hep3B cells assessed as inhibition of hypoxia-induced luciferase expression after 16 hrs by reporter assay [PMID: 17583950]
HepG2 IC50 29.2 μM Antitumor activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay [PMID: 35504209]
KB 3-1 IC50 6.9 μM Cytotoxicity against drug-sensitive human KB-3-1 cells after 48 hrs by MTS/PMS assay [PMID: 11720520]
KB-V1 IC50 7.5 μM Cytotoxicity against multidrug-resistant human KBV1 cells after 48 hrs by MTS/PMS assay [PMID: 11720520]
MIA PaCa-2 IC50 5.8 μM Cytotoxicity against human MIAPaCa2 cells after 24 hrs by MTT assay [PMID: 21775156]
Vero C1008 CC50 > 300 μM Cytotoxicity against African green monkey Vero E6 cells assessed as cell viability treated for 24 hrs by CCK8 assay [PMID: 35620927]

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In Vitro Studies

Cryptotanshinone reduced viability and colony formation in A498, 786-O and ACHN renal carcinoma cells. Responses varied by concentration, exposure time and cell line; ACHN cells were less sensitive than A498 and 786-O cells under the reported conditions. [2]

STAT3 phosphorylation and SHP-2 activity in U251 cells

Cell-based study · Human U251 glioma cells and SHP-2 immunocomplexes recovered from treated-cell lysates [1]

CTS reduced STAT3 Tyr705 phosphorylation while total STAT3 and Ser727 phosphorylation were comparatively unchanged. Treated-cell SHP-2 phosphatase activity increased. NSC-87877 counteracted both effects, supporting involvement of SHP-1/2-sensitive phosphatase signaling without establishing direct binding of CTS to STAT3 or SHP-2.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
STAT3 Tyr705 and Ser727 phosphorylation; total STAT3Reported qualitative result Tyr705 phosphorylation decreased with concentration and time; no significant Ser727 effect reported. Caption: mean±S.E.M., n=3 per group.[1]
SHP-2-associated phosphatase activity in treated-cell lysatesReported qualitative result Activity increased at 5 and 10 μM CTS; 25 μM NSC-87877 counteracted the CTS-associated activity increase and restored p-STAT3 toward control. Caption: mean±S.E.M., n=3 per group.[1]

Literature-Reported Treatment Conditions

Treatment concentration
CTS 0, 1.25, 2.5, 5, 10 and 20 μM in Figure 3a; 10 μM in the Figure 3b time course. Figure 4f: 0, 5 and 10 μM CTS. Figure 4g–h: 10 μM CTS with or without 25 μM NSC-87877.
Exposure duration
Figure 3a and Figure 4f: 2 h CTS; Figure 3b: 0, 0.25, 0.5, 1, 2 and 4 h. Figure 4g–h: 30 min NSC-87877 pretreatment followed by 120 min CTS.
Method
Cell treatment followed by western blot or SHP-2 immunocomplex phosphatase activity measurement; 0 μM CTS and inhibitor-alone conditions shown.
Co-treatment
NSC-87877 only in the mechanistic inhibitor comparison; its combination results are not CTS-alone effects.
Reported limits
Final solvent composition for these panels is not specified in the retrieved caption/reagent methods. Caption n=3 is retained without assigning a biological replicate unit.
Methods and source locations

Compound reported in the paper: Cryptotanshinone; Compound label in the paper: CTS

Evidence concerns the reported cryptotanshinone material; it does not validate an Adooq lot, purity or stereochemical composition.

Figures 3a–b and 4f–h; Chemicals, reagents and antibodies; SHP-2 PTP activity assay; Statistical analysis

STAT3 Tyr705 and Ser727 phosphorylation; total STAT3: Western blotting and densitometry — Figure 3a–b, Results: suppression of STAT3 activation

SHP-2-associated phosphatase activity in treated-cell lysates: SHP-2 immunoprecipitation followed by tyrosine phosphatase assay; paired western blots — Figure 4f–h and caption; SHP-2 PTP activity assay

RCC viability and colony formation under cryptotanshinone treatment

Cell-based study · Human A498, 786-O and ACHN renal cell carcinoma cell lines [2]

CCK-8 viability decreased with treatment concentration and time, and subsequent colony formation was reduced. ACHN cells were less sensitive than A498 and 786-O cells under the reported conditions. These are cell-based endpoints rather than a biochemical STAT3 IC50.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
CCK-8 cell viability and colony formationReported qualitative result Concentration- and time-associated reduction in viability; colony numbers decreased after 48 h exposure followed by 8 days in normal medium. Figure 1 caption: mean ± SD, n = 3.[2]

Literature-Reported Treatment Conditions

Treatment concentration
CCK-8: A498 and 786-O, 0.5, 1, 2.5, 5, 7.5 and 10 μM; ACHN, 1, 2.5, 5, 10, 15 and 20 μM, each with control. Colonies: A498, 0.25, 0.5, 0.75 and 1 μM; 786-O, 0.25, 0.5, 1 and 1.5 μM; ACHN, 1, 2.5 and 5 μM, each with control.
Exposure duration
CCK-8: 24, 48 and 72 h. Colony formation: 48 h treatment, then 8 days in normal medium.
Method
Single-compound treatment versus DMSO vehicle. CCK-8 method specifies five replicate wells per concentration; caption n=3 and general statement of at least three independent experiments are separately retained.
Vehicle
DMSO; final concentration not specified in the retrieved methods.
Reported limits
No fitted IC50 is extracted; final DMSO percentage and per-panel biological replicate definitions are not specified.
Methods and source locations

Compound reported in the paper: Cryptotanshinone; Compound label in the paper: CPT

Evidence concerns the reported cryptotanshinone material; it does not validate an Adooq lot, purity or stereochemical composition.

Figure 1A–G and caption; Antibodies and reagents; Cell culture; CCK-8 assays; Colony formation assays; Statistical analysis

CCK-8 cell viability and colony formation: CCK-8 absorbance at 450 nm; crystal-violet colony counting (>50 cells per colony) — Figure 1B–G and caption; CCK-8 and colony formation methods

In Vivo Studies

In male athymic nude mice with established A498 xenografts, cryptotanshinone at 5 mg/kg intraperitoneally every other day for 18 days reduced tumor growth and terminal tumor weight versus vehicle (n=6 per group). Body weight was reported unaffected; this endpoint alone does not establish safety. [2]

Cryptotanshinone in an established A498 RCC xenograft model

Animal study · Five-week-old male athymic nude mice bearing established subcutaneous A498 RCC xenografts; n=6 per group [2]

CPT reduced tumor growth and terminal tumor weight relative to vehicle without a reported body-weight difference. This is a single immunodeficient mouse xenograft study, with no demonstrated clinical efficacy or comprehensive safety conclusion.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
Tumor volume, terminal tumor weight and body weightReported qualitative result Lower tumor volume and tumor weight; tumor-volume difference around day 12, P < 0.05; body weight reported unaffected. n=6 per group, mean ± SD per caption.[2]

Conditions shared by the study groups

Route
Intraperitoneal injection
Frequency
Every other day
Treatment course
18 days of treatment; all mice sacrificed at day 20 according to Methods
Vehicle
10% DMSO + 30% PEG 300 + 5% Tween 80 + ddH2O
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
CPT 5 mg/kg versus matched vehicle
5 mg/kg		Matched vehicle, n=6; groups randomized at approximately 300 mm³ tumor volume.Tumor volume and terminal tumor weight were lower with CPT; volume differences were reported from around day 12 (P < 0.05). Body weight was reported unaffected. Figure 6 caption: mean ± SD, *P < 0.05, **P < 0.01 versus control.[2]
CPT 5 mg/kg versus matched vehicle
Model: Five-week-old male athymic nude mice bearing established subcutaneous A498 RCC xenografts; n=6 per group
Reported limits: No exact tumor-volume or weight effect size extracted from the plot; no comprehensive toxicity or survival assessment established by these endpoints.
Methods and source locations

Compound reported in the paper: Cryptotanshinone; Compound label in the paper: CPT

Evidence concerns the reported cryptotanshinone material; it does not validate an Adooq lot, purity or stereochemical composition.

Figure 6A–C and caption; Results: CPT attenuated cell growth while activated cell apoptosis in vivo; Xenograft studies

Tumor volume, terminal tumor weight and body weight: Caliper-derived tumor volume, tumor weighing and body-weight monitoring — Figure 6A–C and caption; Xenograft studies; associated Results paragraph

CPT 5 mg/kg versus matched vehicle · Figure 6A–C and caption; Results: CPT attenuated cell growth while activated cell apoptosis in vivo; Xenograft studies

Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 35825-57-1
Applications Stat3 inhibitor
Formula C19H20O3
Molecular Weight 296.4
Synonyms Tanshinone
SMILES
C[C@H]1COC2=C1C(=O)C(=O)C3=C2C=CC4=C3CCCC4(C)C

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO Warmed: 5 mg/mL (16.87 mM)
Water Insoluble
Ethanol Warmed: 1 mg/mL (3.37 mM)

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

In Vivo Preparation

Concentration
1.18 mg/mL
Vehicle
5% DMSO+40%PEG 300+5% Tween80 +ddH2O

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Research References

  1. [1] Liang Lu, Sulin Zhang, Cuixian Li, et al. Cryptotanshinone inhibits human glioma cell proliferation in vitro and in vivo through SHP-2-dependent inhibition of STAT3 activation Cell Death & Disease (2017). PMID: 28492557 DOI: 10.1038/cddis.2017.174 Source material
  2. [2] Zhiguo Chen, Rujian Zhu, Jiayi Zheng, et al. Cryptotanshinone inhibits proliferation yet induces apoptosis by suppressing STAT3 signals in renal cell carcinoma Oncotarget (2017). PMID: 28654902 DOI: 10.18632/oncotarget.18483 Source material

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