Nutrabiotech Gedatolisib 98% 3G Powder, PF-05212384 PKI-587 compound, high purity dual PI3K mTOR inhibitor, PAM pathway blocker, tumor anti-proliferation research raw material

Gedatolisib CAS 1197160-78-3 High-Purity Powder Multi-Target PI3K/mTOR Dual Inhibitor PAM Pathway Blocker Anti-Tumor Biochemical Research Reagent

High-purity Gedatolisib powder CAS 1197160-78-3 is a potent, multi-target small-molecule PAM pathway inhibitor. It comprehensively blocks all class I PI3K isoforms (α, β, γ, δ) and dual mTOR complexes (mTORC1/mTORC2), effectively suppressing downstream AKT oncogenic signaling. Unlike single-target PI3K inhibitors, Gedatolisib delivers broader and more durable pathway suppression, inhibiting tumor cell proliferation and inducing apoptosis. Widely applied in laboratory research of HR+/HER2- breast cancer, PIK3CA wild-type/mutant tumor models, endocrine resistance mechanism exploration, and targeted anti-cancer drug screening. All batches support strict HPLC purity testing, customized packaging and global bulk supply for oncology pharmacology laboratories. For scientific research use only.

 

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Gedatolisib (CAS 1197160-78-3) Dual PI3K/mTOR Inhibitor | PF-05212384 / PKI-587, Pan-PI3K & mTORC1/2 Kinase Inhibitor for Oncology

Gedatolisib CAS 1197160-78-3
Dual PI3K / mTOR Kinase Inhibitor (PF-05212384, PKI-587)

Gedatolisib (CAS 1197160-78-3), also PF-05212384 / PKI-587, is a potent, balanced dual inhibitor of class I PI3K isoforms and mTOR kinase with cellular IC50s of ~0.4 nM (PI3Kalpha), 5.4 nM (PI3Kgamma) and 1.6 nM (mTOR). It simultaneously shuts down both arms of the PI3K/Akt/mTOR oncogenic axis. Molecular formula C32H41N9O4, MW 615.73. Research-grade with COA.

Dual PI3K/mTOR PF-05212384 PKI-587 Pan-PI3K mTORC1/2 Oncology PI3K/Akt/mTOR Breast Cancer
Request a Quote Technical Specs
615.73
MW (C32H41N9O4)
1.6 nM
mTOR IC50
PI3K + mTOR
Dual blockade

Molecular Information

Name: Gedatolisib
CAS: 1197160-78-3
Formula: C32H41N9O4
MW: 615.73 g/mol
Class: Morpholino-triazine bis-urea
Core: Dimorpholino-triazinyl bis-aryl urea
Target: PI3K (class I) + mTOR
IC50: PI3Ka 0.4 / mTOR 1.6 nM
Appearance: White solid powder
Synonyms: PF-05212384 / PKI-587
Storage: -20 C
🧪
CAS Number
1197160-78-3
⚖️
Molecular Weight
615.73
🎯
Primary Activity
Dual PI3K/mTOR
✅
Purity
≥98%

Product Technical Specifications

Complete physicochemical properties and QC parameters for Gedatolisib (CAS 1197160-78-3)

📋 Physicochemical Properties

  • Product NameGedatolisib
  • IUPAC Core1-[4-[[4-(dimethylamino)-1-piperidinyl]carbonyl]phenyl]-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea
  • CAS Number1197160-78-3
  • SynonymsPF-05212384; PKI-587; PKI587
  • Molecular FormulaC32H41N9O4
  • Molecular Weight615.73 g/mol
  • SourceSynthetic small molecule (Wyeth/Pfizer, now Celcuity)
  • AppearanceWhite to off-white solid
  • Melting PointNot reported (amorphous)
  • Water SolubilityLow (formulate in DMSO/organic)
  • Organic SolubilityDMSO
  • Compound ClassMorpholino-triazine bis-aryl urea / dual PI3K-mTOR inhibitor
  • HS Code2934.99

🔬 Quality Control & Handling

  • Purity (HPLC)≥98%
  • FormSolid powder
  • Primary TargetClass I PI3K (alpha/gamma/delta) + mTOR kinase
  • Pathway Readoutp-AKT, p-S6K, p-4E-BP1, p-PRAS40 down; p-ERK may rise (feedback)
  • SelectivityBalanced PI3K + mTOR; distinct from rapalogs (mTORC1-only)
  • Storage Condition-20 C, sealed, protect from light
  • Solution StabilityAliquot DMSO stocks; avoid freeze-thaw
  • ShippingBlue ice / cold chain recommended
  • QC DocumentationCOA / HPLC / NMR / MS / MSDS
  • Pack Sizes1g / 5g / 10g / 100g / 1KG
  • Stock StatusIn Stock
  • Use StatementResearch use only; not for human/clinical use

Key Molecular Targets & Pathway Nodes

Gedatolisib hits both limbs of the PI3K/Akt/mTOR axis at the kinase level — a broader blockade than rapalogs, which only allosterically inhibit mTORC1.

🧬 PI3Kalpha (p110alpha) 🧬 PI3Kgamma / delta ⚙️ mTOR (mTORC1 & mTORC2) 📈 AKT / PKB 📈 p70S6K / S6 📈 4E-BP1 🔗 PI3K/Akt/mTOR Axis 🧱 PRAS40 / TSC 🧬 PTEN / PIK3CA 🔬 Feedback p-ERK 🩸 Angiogenesis Output 🧫 PI3K-Addicted Tumors

How Gedatolisib Works: Simultaneous PI3K and mTOR Kinase Blockade

Gedatolisib attacks both catalytic nodes of the oncogenic PI3K/Akt/mTOR network

1

PI3K Catalytic Inhibition

Gedatolisib binds the ATP sites of class I PI3K catalytic subunits (most potently p110alpha, also gamma/delta), blocking conversion of PIP2 to PIP3 at the membrane. This starves downstream AKT of its membrane-docking lipid, blunting AKT Thr308 and Ser473 phosphorylation even before mTORC2 is engaged.

2

mTOR Kinase Inhibition

Distinct from rapalogs, gedatolisib directly inhibits the mTOR kinase domain, suppressing both mTORC1 (S6K/4E-BP1) and mTORC2 (AKT Ser473) outputs. This dual coverage avoids the classic rapalog loophole where mTORC2-driven AKT feedback limits efficacy.

3

Collapse of Growth & Survival Signaling

With PI3K and mTOR both suppressed, downstream p70S6K, 4E-BP1 and PRAS40 phosphorylation fall, cap-dependent translation and cell-growth programs stall, and apoptosis/autophagy ensue in PIK3CA- or PTEN-altered cells. Notably, relief of mTORC1 feedback can transiently raise p-ERK, a marker studied in combination strategies.

⚖️ Gedatolisib vs Rapalogs vs Pan-PI3K

  • Gedatolisib (this product)Dual PI3K + mTOR kinase; PI3Ka 0.4 / mTOR 1.6 nM
  • Rapalogs (everolimus)Allosteric mTORC1 only; mTORC2/AKT feedback spared
  • Pan-PI3K (BKM120)PI3K-only; leaves mTOR arm active (feedback)
  • PI3K/mTOR (BEZ235)Dual but less balanced / tolerability-different
  • Net CoverageBroadest single-agent PI3K/Akt/mTOR blockade
  • Research UsePI3K-addicted & resistant solid tumors, combo studies

♻️ Downstream Biological Consequences

  • AKTReduced p-AKT (T308 & S473)
  • Translationp-S6K & p-4E-BP1 suppression
  • Cell CycleG1 arrest; reduced cyclin D1
  • SurvivalApoptosis / autophagy in PIK3CA/PTEN models
  • FeedbackPossible p-ERK rise (combination rationale)
  • AngiogenesisReduced HIF-1alpha / VEGF output

Research Applications & Models

Dual PI3K/mTOR blockade is a flagship strategy in PIK3CA-mutant and PTEN-loss oncology — and a window into resistance and combination science.

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PI3K-Addicted Cancers

Studied in breast, endometrial, ovarian and prostate models bearing PIK3CA mutations or PTEN loss, where gedatolisib's dual blockade collapses the dominant survival axis. A reference dual inhibitor for pathway-addicted lines.

PIK3CA / PTEN
🎀

Breast Cancer Research

Investigated alone and with endocrine therapy, CDK4/6 inhibitors and HER2 blockers in hormone-receptor-positive and HER2+ contexts, probing synthetic-lethal and feedback combinations.

HR+ / HER2
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Resistance & Feedback Studies

Used to dissect mTORC1-release of AKT/ERK feedback that limits rapalogs and pan-PI3K drugs, informing rational combinations with MEK or CDK inhibitors.

Feedback Loops
🩸

Anti-Angiogenic Models

mTOR output controls HIF-1alpha and VEGF; gedatolisib is studied for tumor-vascular normalization and anti-angiogenic effects in xenografts.

HIF-1alpha / VEGF
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PI3K/Akt/mTOR Pathway Tool

A fiducial dual kinase inhibitor for Western panels (p-AKT, p-S6K, p-4E-BP1, p-PRAS40) and for discriminating PI3K-dependent from mTOR-dependent phenotypes.

Pathway Readout
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In Vivo Efficacy Models

Evaluated in subcutaneous and orthotopic xenografts for tumor-growth inhibition, pharmacokinetic/pharmacodynamic (p-S6) correlation and tolerability.

Xenograft PD
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Combination Screening

Deployed in drug-combination matrices with taxanes, anti-HER2, CDK4/6 and MEK inhibitors to identify synergy and mitigate adaptive resistance.

Combo Matrix
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Biomarker Discovery

Paired with genomic/proteomic profiling to find predictors of response (PIK3CA mutation, PTEN loss, AKT activation) for patient-selection research.

Biomarkers

Key Literature & Landmark Publications

Key references on dual PI3K/mTOR inhibition and the gedatolisib clinical program.

Maira SM, et al. Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor. Mol Cancer Ther. 2008;7(7):1851-63. (dual PI3K/mTOR pharmacology).
doi: 10.1158/1535-7163.MCT-08-0018
Serra V, et al. PI3K inhibition results in enhanced HER3 expression in HER2-driven breast tumors. (feedback & dual-inhibitor rationale).
Landmark reference
Courtney KD, et al. PI3K/mTOR double blockade in endogenous tumors. (dual-pathway concept).
Landmark reference
Investigator report. Gedatolisib (PF-05212384) in PIK3CA-altered solid tumors. (Celcuity clinical program).
Landmark reference
Workman P, et al. How much more can we learn from dual PI3K-mTOR inhibitors? (review).
Landmark reference

Available Sizes & Ordering

Research-grade Gedatolisib (CAS 1197160-78-3) with full QC documentation; standard packs and bulk custom quantities supported.

TierPack SizeStock StatusSuitable ForLead Time
Standard1gIn StockPI3K/mTOR cell signaling assaysSame/next-day ship
Medium5gIn StockIn vivo tumor & pathway modelsSame/next-day ship
Large10gIn StockCombination & resistance studiesSame/next-day ship
Bulk100gIn StockFormulation & process developmentQuote to confirm
Industrial1KGMade to orderPilot/production scale, CMO supplyBatch delivery

💡 Reference sizes shown above; for exact pricing and availability please contact us for a quote. Bulk orders qualify for tiered discounts.

Frequently Asked Questions (FAQ)

What is gedatolisib and what pathways does it hit?
Gedatolisib (CAS 1197160-78-3), also PF-05212384 / PKI-587, is a dual inhibitor of class I PI3K isoforms and the mTOR kinase. Cellular IC50s are ~0.4 nM (PI3Kalpha), 5.4 nM (PI3Kgamma) and 1.6 nM (mTOR). Unlike rapalogs it hits the mTOR kinase directly, so it suppresses both mTORC1 and mTORC2. Formula C32H41N9O4, MW 615.73.
How is gedatolisib different from everolimus (a rapalog)?
Everolimus is an allosteric mTORC1-only inhibitor; it spares mTORC2, so AKT (via mTORC2 Ser473) stays active and can drive resistance. Gedatolisib directly inhibits the mTOR kinase (both complexes) and also blocks PI3K upstream, giving broader, more complete suppression of the PI3K/Akt/mTOR axis in a single agent.
Why block PI3K and mTOR at the same time?
The PI3K/Akt/mTOR network is the most commonly activated oncogenic pathway. Blocking only PI3K leaves mTORC1 active and triggers AKT feedback; blocking only mTOR (rapalogs) leaves PI3K/AKT intact. Dual blockade collapses both limbs and reduces the adaptive feedback that limits single-node drugs — the central rationale for gedatolisib and related PI3K/mTOR agents.
What readouts confirm gedatolisib activity?
A Western panel of p-AKT (T308 & S473), p-S6K (Thr389), p-S6 (Ser235/236), p-4E-BP1 and p-PRAS40 shows broad suppression. Expect reduced PI3K and mTOR outputs simultaneously. Note that relieving mTORC1 feedback can transiently raise p-ERK, a marker often used to justify MEK-inhibitor combinations.
In which tumor models is gedatolisib studied?
Primarily PIK3CA-mutant or PTEN-loss cancers — breast (HR+, HER2+), endometrial, ovarian, prostate and other solid tumors — plus combination studies with endocrine therapy, CDK4/6, HER2 and MEK inhibitors. It is a reference dual inhibitor for pathway-addicted cell lines and xenografts.
How soluble is gedatolisib and how should it be prepared?
Gedatolisib is soluble in DMSO (formulate stock there) and has limited aqueous solubility, so in vivo work typically uses suspension or co-solvent formulations. For cell assays dilute the DMSO stock into medium keeping final DMSO ≤0.1% v/v; typical active concentrations are low nanomolar to low micromolar. Store solid at -20 C and aliquot stocks.
Is QC documentation provided?
Every batch ships with a Certificate of Analysis (COA) including HPLC purity, NMR structural confirmation and MS data. MSDS/SDS, residual-solvent data and Certificates of Origin are available on request. Sample evaluation is available for qualified institutions — please contact us.

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Research-grade Gedatolisib (CAS 1197160-78-3) — purity ≥98% HPLC, COA included
PF-05212384 / PKI-587 — simultaneous PI3K + mTOR kinase blockade for PI3K-addicted oncology — request a quote today

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Weight 1 g

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