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Fig. 1 · Structure
Cat. No.
A11161
CAS No.
19545-26-7
Formula
C23H24O8
Mol. Weight
428.43

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Wortmannin

Cat. No. A11161 CAS 19545-26-7

PI3K inhibitor

Wortmannin is a potent, selective, cell-permeable and irreversible inhibitor of phosphatidylinositol 3-kinase (PI 3-kinase) (IC50 = 2 - 4 nM) which also potently inhibits polo-like kinase 1 (PLK1) (IC50 = 5.8 nM).

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Publications for Wortmannin

2 publications citing this product

  1. Weili Chen, .et al. , Communications Biology, 2024, 7:488 PMID: 38649462
  2. Hirotake Ishida, .et al. , J Neurosci, 2021, Oct 13;41(41):8494-8507 PMID: 34452938
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Biological Activity

Target & Activity

Target Activity Value
PI3K (Cell-free assay) 3 nM
DNA-PK [12](Cell-free assay) 16 nM
ATM [12](Cell-free assay) 150 nM
MLCK (Cell-free assay) 170 nM
ATR [12](Cell-free assay) 1.8 μM

Cellular Effect

Cell Line Activity Value Description Reference
A549 IC50 0.22 μM Inhibition of Plk3 in human A549 cells assessed as casein substrate phosphorylation by Western blot [PMID: 17135248]
A549 IC50 11.4 μM Antiproliferative activity against human A549 cells after 48 hrs by SRB method [PMID: 18630894]
A549 IC50 4.28 ng/mL Cytotoxicity against human A549 cells after 24 hrs by YO-PRO-1 assay [PMID: 19138858]
A549 IC50 4.28 ng/mL Cytotoxicity against human A549 cells after 24 hrs by propidium iodide assay [PMID: 19138858]
HeLa IC50 49 nM Inhibition of AX-7503 binding to recombinant Plk3 expressed in HeLa cells by Western blot [PMID: 17135248]
MCF7 IC50 > 100 μM Cytotoxicity against human MCF7 cells after 72 hrs by MTS/PMS assay [PMID: 23040731]
Sf9 IC50 0.012 μM Inhibition of human PI3Kalpha expressed in Sf9 cells by fluorescent polarization assay [PMID: 21121631]

In Vivo Studies

In KB xenograft-bearing mice, Cremophor-solubilized wortmannin had little effect alone but delayed tumor growth when combined with irradiation. Encapsulated wortmannin produced a greater delay with irradiation, demonstrating that the result depended on formulation and combination treatment. [1]

A separate acute CD1 mouse experiment reported higher ALT and lower granulocyte counts with Cremophor-solubilized wortmannin than with the nanoparticle formulation at the matched 0.14 mg/kg drug dose. These findings limit extrapolation between formulations. [1]

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

Acute blood and liver-marker responses to two wortmannin formulations

Animal study · Non-tumor-bearing CD1 mice [1]

At matched reported wortmannin doses, Table 2 shows higher ALT and lower granulocyte counts with the Cremophor formulation than with NP Wtmn at 0.14 mg/kg. The lower 0.07 mg/kg groups are retained in the same experiment. Normal ranges are reference ranges, not an untreated cohort.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
Plasma alanine transaminase at 0.14 mg/kg wortmanninreported observation Wtmn: 134 ± 17 U/L; NP Wtmn: 82 ± 12 U/L; reported normal range: 40–50 U/L[1]
Granulocyte count at 0.14 mg/kg wortmanninreported observation Wtmn: 0.8 ± 0.14 (10^3/μL); NP Wtmn: 2.9 ± 0.07 (10^3/μL); reported normal range: 1.2–8 (10^3/μL)[1]
Plasma alanine transaminase at 0.07 mg/kg wortmanninreported observation Wtmn: 64 ± 11 U/L; NP Wtmn: 60 ± 9 U/L; reported normal range: 40–50 U/L[1]
Granulocyte count at 0.07 mg/kg wortmanninreported observation Wtmn: 2.4 ± 0.11 (10^3/μL); NP Wtmn: 3.7 ± 0.12 (10^3/μL); reported normal range: 1.2–8 (10^3/μL)[1]

Conditions shared by the study groups

Route
Tail-vein intravenous injection
Frequency
Single injection
Treatment course
24 h observation before blood profiling
Vehicle
Cremophor formulation for unencapsulated wortmannin; lipid-polymer nanoparticles for NP Wtmn
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
Wtmn, higher dose
0.14 mg/kg wortmannin		Matched NP Wtmn dose; published normal rangesALT 134 ± 17 U/L; granulocytes 0.8 ± 0.14 (10^3/μL).[1]
NP Wtmn, higher dose
0.14 mg/kg wortmannin equivalent; authors report 7 mg/kg NP Wtmn		Wtmn at the matched reported drug doseALT 82 ± 12 U/L; granulocytes 2.9 ± 0.07 (10^3/μL).[1]
Wtmn, lower dose
0.07 mg/kg wortmannin		Matched NP Wtmn dose; published normal rangesALT 64 ± 11 U/L; granulocytes 2.4 ± 0.11 (10^3/μL).[1]
NP Wtmn, lower dose
0.07 mg/kg wortmannin equivalent		Wtmn at the matched reported drug doseALT 60 ± 9 U/L; granulocytes 3.7 ± 0.12 (10^3/μL).[1]
Wtmn, higher dose
Model: CD1 mice
Reported limits: Group n is not given in the retrieved main-text experiment description. Exact Cremophor composition is not specified there.
NP Wtmn, higher dose
Model: CD1 mice
Reported limits: Group n is not given in the retrieved main-text experiment description. Exact Cremophor composition is not specified there.
Wtmn, lower dose
Model: CD1 mice
Reported limits: Group n is not given in the retrieved main-text experiment description. Exact Cremophor composition is not specified there.
NP Wtmn, lower dose
Model: CD1 mice
Reported limits: Group n is not given in the retrieved main-text experiment description. Exact Cremophor composition is not specified there.
Methods and source locations

Compound reported in the paper: Wortmannin; Compound label in the paper: Wtmn (Cremophor-solubilized); NP Wtmn (encapsulated comparator)

Evidence concerns the reported wortmannin formulations and mouse models; the nanoparticle preparation is not A11161, and these results do not validate an Adooq lot.

Table 2 including footnote; Results: NP Wtmn Has Significantly Lower Toxicity than Wtmn; Materials and Methods: Materials, Toxicity

Plasma alanine transaminase at 0.14 mg/kg wortmannin: Blood profile 24 h after a single tail-vein intravenous injection; values transcribed from Table 2. The main table does not define the ± statistic or group n. — Table 2: 1/5th MTD, ALT row

Granulocyte count at 0.14 mg/kg wortmannin: Blood profile 24 h after a single tail-vein intravenous injection; values transcribed from Table 2. The main table does not define the ± statistic or group n. — Table 2: 1/5th MTD, Granulocytes row

Plasma alanine transaminase at 0.07 mg/kg wortmannin: Blood profile 24 h after a single tail-vein intravenous injection; values transcribed from Table 2. The main table does not define the ± statistic or group n. — Table 2: 1/10th MTD, ALT row

Granulocyte count at 0.07 mg/kg wortmannin: Blood profile 24 h after a single tail-vein intravenous injection; values transcribed from Table 2. The main table does not define the ± statistic or group n. — Table 2: 1/10th MTD, Granulocytes row

Wtmn, higher dose · Table 2 and footnote; Materials and Methods: Toxicity

NP Wtmn, higher dose · Table 2 and footnote; Materials and Methods: Toxicity

Wtmn, lower dose · Table 2 and footnote; Materials and Methods: Toxicity

NP Wtmn, lower dose · Table 2 and footnote; Materials and Methods: Toxicity

Wortmannin formulation and radiotherapy in KB xenografts

Animal study · KB subcutaneous xenografts in 6–8-week-old male NOD/SCID mice [1]

The drug-only groups tracked the untreated group. Both wortmannin formulations plus irradiation delayed tumor growth, with greater delay for NP Wtmn plus irradiation. The paper reports P < 0.01 for comparison of the two combination groups. This supports a formulation- and combination-dependent result in this xenograft model.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
Serial percentage change in tumor volumeTumor growth delay Wtmn alone and NP Wtmn alone: minimal effect; both plus XRT: delayed growth; NP Wtmn + XRT versus Wtmn + XRT: P < 0.01 (reported).[1]
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
No treatmentComparator for all interventionsRapid tumor growth in the displayed follow-up.[1]
XRT aloneNo-treatment and combination groupsTumor growth delay less marked than the drug-plus-XRT groups.[1]
Wtmn alone
0.07 mg/kg wortmannin		No treatment and Wtmn + XRTMinimal antitumor effect alone.[1]
NP Wtmn alone
3.5 mg/kg NP Wtmn, reported equivalent to 0.07 mg/kg wortmannin		No treatment and NP Wtmn + XRTMinimal antitumor effect alone.[1]
Wtmn + XRT
0.07 mg/kg wortmannin		XRT alone, Wtmn alone and NP Wtmn + XRTTumor growth delay; less delay than NP Wtmn + XRT.[1]
NP Wtmn + XRT
3.5 mg/kg NP Wtmn, reported equivalent to 0.07 mg/kg wortmannin		XRT alone, NP Wtmn alone and Wtmn + XRTGreater tumor growth delay than Wtmn + XRT (reported P < 0.01).[1]
No treatment
Model: KB subcutaneous xenografts in 6–8-week-old male NOD/SCID mice
Reported limits: Group n is not given in the retrieved main-text experiment description.
XRT alone
Model: KB subcutaneous xenografts in 6–8-week-old male NOD/SCID mice
Route: Local tumor irradiation
Frequency: One exposure
Treatment course: 6 Gy irradiation
Reported limits: Group n is not given in the retrieved main-text experiment description. Exact Cremophor composition is not specified there.
Wtmn alone
Model: KB subcutaneous xenografts in 6–8-week-old male NOD/SCID mice
Route: Tail-vein intravenous injection
Frequency: Single injection
Vehicle: Cremophor formulation for unencapsulated wortmannin; lipid-polymer nanoparticles for NP Wtmn
Reported limits: Group n is not given in the retrieved main-text experiment description. Exact Cremophor composition is not specified there.
NP Wtmn alone
Model: KB subcutaneous xenografts in 6–8-week-old male NOD/SCID mice
Route: Tail-vein intravenous injection
Frequency: Single injection
Vehicle: Cremophor formulation for unencapsulated wortmannin; lipid-polymer nanoparticles for NP Wtmn
Reported limits: Group n is not given in the retrieved main-text experiment description. Exact Cremophor composition is not specified there.
Wtmn + XRT
Model: KB subcutaneous xenografts in 6–8-week-old male NOD/SCID mice
Route: Tail-vein intravenous injection
Frequency: Single injection
Treatment course: Local 6 Gy irradiation 3 h after injection
Vehicle: Cremophor formulation for unencapsulated wortmannin; lipid-polymer nanoparticles for NP Wtmn
Reported limits: Group n is not given in the retrieved main-text experiment description. Exact Cremophor composition is not specified there.
NP Wtmn + XRT
Model: KB subcutaneous xenografts in 6–8-week-old male NOD/SCID mice
Route: Tail-vein intravenous injection
Frequency: Single injection
Treatment course: Local 6 Gy irradiation 3 h after injection
Vehicle: Cremophor formulation for unencapsulated wortmannin; lipid-polymer nanoparticles for NP Wtmn
Reported limits: Group n is not given in the retrieved main-text experiment description. Exact Cremophor composition is not specified there.
Methods and source locations

Compound reported in the paper: Wortmannin; Compound label in the paper: Wtmn (Cremophor-solubilized) and NP Wtmn comparator

Evidence concerns the reported wortmannin formulations and mouse models; the nanoparticle preparation is not A11161, and these results do not validate an Adooq lot.

Figure 5A and caption; Results: NP Wtmn Is an Effective Radiosensitizer in Vivo; Materials and Methods: Materials, Tumor Efficacy, Statistics

Serial percentage change in tumor volume: Caliper tumor measurements every 2–4 days; reported combination comparison used area under the growth curve over days 0–76 and an exact one-sided Wilcoxon rank sum test. No curve-derived numerical efficacy estimate extracted. — Figure 5A; Results: NP Wtmn Is an Effective Radiosensitizer in Vivo; Materials and Methods: Tumor Efficacy, Statistics

No treatment · Figure 5A and caption; Results: NP Wtmn Is an Effective Radiosensitizer in Vivo; Materials and Methods: Tumor Efficacy

XRT alone · Figure 5A and caption; Results: NP Wtmn Is an Effective Radiosensitizer in Vivo; Materials and Methods: Tumor Efficacy

Wtmn alone · Figure 5A and caption; Results: NP Wtmn Is an Effective Radiosensitizer in Vivo; Materials and Methods: Tumor Efficacy

NP Wtmn alone · Figure 5A and caption; Results: NP Wtmn Is an Effective Radiosensitizer in Vivo; Materials and Methods: Tumor Efficacy

Wtmn + XRT · Figure 5A and caption; Results: NP Wtmn Is an Effective Radiosensitizer in Vivo; Materials and Methods: Tumor Efficacy

NP Wtmn + XRT · Figure 5A and caption; Results: NP Wtmn Is an Effective Radiosensitizer in Vivo; Materials and Methods: Tumor Efficacy

Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 19545-26-7
Applications PI3K inhibitor
Formula C23H24O8
Molecular Weight 428.43
Synonyms SL-2052
SMILES
CC(=O)O[C@@H]1C[C@]2([C@@H](CCC2=O)C3=C1[C@]4([C@H](OC(=O)C5=COC(=C54)C3=O)COC)C)C

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO 73 mg/mL (170.38 mM)
Water Insoluble
Ethanol Insoluble

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
4 mg/mL
Vehicle
5% DMSO+40% PEG 300+5% Tween 80+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] Shrirang Karve, Michael E. Werner, Rohit Sukumar, et al. Revival of the abandoned therapeutic wortmannin by nanoparticle drug delivery. Proceedings of the National Academy of Sciences of the United States of America (2012). PMID: 22547809 DOI: 10.1073/pnas.1120508109 Source material

Publications

2 publications citing this product

  1. Weili Chen, .et al. , Communications Biology, 2024, 7:488 PMID: 38649462
  2. Hirotake Ishida, .et al. , J Neurosci, 2021, Oct 13;41(41):8494-8507 PMID: 34452938

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