Fedratinib CAS 936091‑26‑8 99% High‑Purity Powder Selective JAK2 Inhibitor TG‑101348 Myeloproliferative Neoplasms

High‑purity 99% Fedratinib crystalline powder CAS 936091‑26‑8, selective JAK2 kinase inhibitor TG‑101348 for myelofibrosis and hematology oncology research.

Fedratinib (Inrebic) CAS 936091-26-8 | Selective JAK2 Inhibitor | Nutrabiotech Chem

Fedratinib (Inrebic) CAS 936091-26-8
Selective JAK2 Inhibitor for Myelofibrosis & JAK-STAT Research

Fedratinib (CAS 936091-26-8), marketed as Inrebic and formerly known as SAR302503, is a potent, selective JAK2 kinase inhibitor with activity against JAK2 V617F and FLT3. By blocking JAK2-driven STAT3/STAT5 phosphorylation it suppresses proliferation and induces apoptosis in myeloproliferative-neoplasm models. Formula C27H36N6O3S, MW 524.69. Research grade with COA.

FedratinibInrebicSAR302503JAK2JAK2 V617FMyelofibrosisJAK-STATFLT3Kinase inhibitorMPN
524.69
MW (C27H36N6O3S)
≥98%
Purity (HPLC)
JAK2
Primary target

Molecular Information

Name: Fedratinib (Inrebic)
CAS: 936091-26-8
Formula: C27H36N6O3S
MW: 524.69 g/mol
Class: Pyrimidine sulfonamide JAK2 inhibitor
Core: 2-aminopyrimidine benzenesulfonamide
Target: JAK2 (V617F) / FLT3
IC50: JAK2 ≈ 3 nM
Activity: STAT3/STAT5 inhibition, anti-proliferative
Form: Free base (dihydrochloride salt available)
Appearance: White to off-white powder
Synonyms: Inrebic; SAR302503
Storage: -20°C, dry, protect from light
936091-26-8
🧪
CAS Number
524.69
⚖️
Molecular Weight
JAK2 Inhibitor
🎯
Primary Activity
≥98%
Purity

Product Technical Specifications

Complete physicochemical properties and QC parameters for Fedratinib (Inrebic, CAS 936091-26-8)

📋 Physicochemical Properties

  • Product NameFedratinib (Inrebic)
  • IUPAC NameN-tert-butyl-3-[[5-methyl-2-[4-(2-pyrrolidin-1-ylethoxy)anilino]pyrimidin-4-yl]amino]benzenesulfonamide
  • CAS Number936091-26-8
  • SynonymsInrebic; SAR302503
  • Molecular FormulaC27H36N6O3S
  • Molecular Weight524.69 g/mol
  • SourceSynthetic (small-molecule kinase inhibitor)
  • AppearanceWhite to off-white powder
  • Water SolubilityLow (free base); dihydrochloride salt improves aqueous solubility
  • Organic SolubilityDMSO (fresh stock, sonication); limited aqueous solubility
  • Boiling PointNot reported (solid)
  • DensityNot reported (solid)
  • Compound ClassPyrimidine sulfonamide JAK2 inhibitor
  • HS Code2935.00

🔬 Quality Control & Handling

  • Purity (HPLC)≥98%
  • FormPowder (research grade)
  • Primary TargetJAK2 (V617F) / FLT3
  • Assay ReadoutSTAT3/STAT5 phosphorylation; proliferation & apoptosis
  • SelectivityJAK2 vs JAK1 35×; JAK3 334×; TYK2 >100×
  • Storage Condition-20°C, sealed, dry, protect from light
  • Solution StabilityDMSO stock stable at -20°C; avoid freeze-thaw
  • ShippingCold chain recommended
  • QC DocumentationCOA / HPLC / NMR / MS / MSDS
  • Pack Sizes5 mg / 25 mg / 100 mg / 500 mg / 1 g
  • Stock StatusIn Stock
  • Use StatementResearch use only; not for human therapeutic or veterinary use

Key Molecular Targets & Biology Nodes

Fedratinib engages the JAK-STAT signaling axis and myeloproliferative-neoplasm biology that define its research utility.

🧬 JAK2 (Janus kinase 2) 🧬 JAK2 V617F mutant 🧬 STAT3 / STAT5 🧬 FLT3 🧭 JAK-STAT pathway 🧬 Myelofibrosis (MF) 🧬 Myeloproliferative neoplasm (MPN) 💥 Cytokine signaling (IL-6, EPO) 🩸 Splenomegaly models 🔬 Hematologic oncology

How Fedratinib Works: Selective JAK2 Blockade of MPN Signaling

Fedratinib targets the JAK2 kinase and downstream STAT transcription factors that drive myeloproliferative-neoplasm survival and proliferation.

1

Selective JAK2 Inhibition

Fedratinib is an ATP-competitive, JAK2-selective inhibitor (JAK2 IC50 ≈ 3 nM) that potently blocks wild-type and V617F-mutant JAK2, with >35–334× selectivity over JAK1/JAK3/TYK2 and retained activity against FLT3.

2

Suppression of STAT3/STAT5 Phosphorylation

With JAK2 blocked, phosphorylation of downstream STAT3 and STAT5 falls, interrupting the constitutive proliferative signaling that sustains myeloproliferative-neoplasm cell survival.

3

Reduced Proliferation & Induced Apoptosis

In JAK2/FLT3-driven models fedratinib suppresses cell proliferation, promotes apoptosis, and in myelofibrosis models reduces splenomegaly and marrow fibrosis.

⚖️ Fedratinib vs Comparators

  • Fedratinib (this product)Selective JAK2; IC50 ~3 nM; FLT3 active; V617F coverage
  • RuxolitinibJAK1/JAK2 (less JAK2-selective); first-in-class MF
  • PacritinibJAK2/FLT3 (also ACVR1)
  • Selective EdgeJAK2-preferential; option after ruxolitinib
  • Research NicheMPN / myelofibrosis models

♻️ Downstream Biological Consequences

  • EnzymeJAK2 kinase down
  • PathwaySTAT3/STAT5 phosphorylation reduced
  • ProliferationJAK2/FLT3-driven cells suppressed
  • ApoptosisIncreased in mutant-driven lines
  • TissueSplenomegaly / fibrosis reduced (models)
  • ModelsMyelofibrosis; PV/ET-post MPN

Research & Application Areas

Fedratinib is a core tool for myelofibrosis, JAK2 V617F and JAK-STAT signaling research.

🧬

Myelofibrosis (MF) Research

Core tool for intermediate/high-risk MF and JAK2 V617F myeloproliferative models.

Myelofibrosis
🧪

JAK2 V617F Models

Proliferation/apoptosis and signaling studies in V617F-driven cell lines.

JAK2 V617F
📡

JAK-STAT Signaling

STAT3/STAT5 phosphorylation readouts and pathway mapping.

JAK-STAT
💊

Kinase Inhibitor Screens

Selectivity panels vs JAK1/JAK3/TYK2 and FLT3.

Selectivity
🩸

Hematologic MPN Studies

PV/ET-post myelofibrosis, splenomegaly and fibrosis endpoints.

MPN
🔬

Drug-Combination / Comparator

Head-to-head with ruxolitinib; post-ruxolitinib resistance research.

Comparator

Key Literature & Landmark Publications

Landmark and representative work on fedratinib / selective JAK2 inhibition and myelofibrosis.

Phase III randomized trial. Fedratinib versus placebo in intermediate-2 / high-risk myelofibrosis (JAKARTA).
Landmark reference
Phase II study. Fedratinib after ruxolitinib failure in myelofibrosis (JAKARTA-2).
Landmark reference
Preclinical selectivity. SAR302503 / fedratinib as a selective JAK2 inhibitor (wild-type and V617F).
Landmark reference
Regulatory. U.S. FDA approval of INREBIC (fedratinib) for myelofibrosis, 2019.
Landmark reference
Safety context. Boxed warning — encephalopathy including Wernicke's; thiamine monitoring guidance.
Landmark reference

Available Sizes & Ordering

Research-grade Fedratinib (CAS 936091-26-8) with full QC documentation; standard packs and bulk custom quantities supported.

TierPack SizeStock StatusSuitable ForLead Time
Standard5 mgIn StockLab screening / assay calibrationSame/next-day ship
Medium25 mgIn StockDose-response / cell assaysSame/next-day ship
Large100 mgIn StockIn vivo / extended studiesSame/next-day ship
Bulk500 mgIn StockLead optimizationQuote to confirm
Industrial1 g+Made to orderProcess developmentBatch 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 Fedratinib and what is it used for?
Fedratinib (CAS 936091-26-8), marketed as Inrebic and formerly known as SAR302503, is a selective JAK2 inhibitor used in myelofibrosis and JAK-STAT signaling research. It inhibits JAK2 (including the V617F mutant) and FLT3, blocking STAT3/STAT5 signaling. Formula C27H36N6O3S, MW 524.69. Supplied as research-grade material with COA.
How does Fedratinib work (mechanism of action)?
Fedratinib is an ATP-competitive, JAK2-selective inhibitor (reported JAK2 IC50 ~3 nM) that blocks both wild-type and V617F-mutant JAK2, reducing phosphorylation of STAT3 and STAT5. This suppresses proliferation and induces apoptosis in JAK2/FLT3-driven cells, and it also retains activity against FLT3.
How selective is Fedratinib for JAK2 versus other JAK family kinases?
Fedratinib is JAK2-preferential: reported selectivity of ~35x over JAK1, ~334x over JAK3, and >100x over TYK2, while retaining FLT3 activity. This distinguishes it from broader JAK1/JAK2 inhibitors such as ruxolitinib, making it valuable for isolating JAK2-specific effects in MPN research.
How soluble is Fedratinib and how should it be prepared?
The free base is soluble in DMSO (prepare fresh stock; sonication recommended) with limited aqueous solubility; the dihydrochloride salt form offers improved water solubility. Store DMSO stocks at -20°C and avoid repeated freeze-thaw cycles. Handling is for research use only.
Is this the same as the approved Inrebic drug?
Inrebic is the FDA-approved fedratinib dihydrochloride capsule (approved in 2019 for intermediate-2 or high-risk myelofibrosis). The material offered here is research-grade fedratinib for laboratory use only and is not a pharmaceutical product. As background, clinical Inrebic carries a boxed warning for encephalopathy including Wernicke's (thiamine deficiency) requiring thiamine monitoring — this is context only, not usage guidance.
Is QC documentation provided?
Every batch ships with a Certificate of Analysis (COA) including HPLC purity, structural confirmation and identity data; MSDS/SDS is included and additional spectra (NMR/MS) are available on request.

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