Nutrabiotech Upadacitinib 98% 1G Powder, 98% high purity Upadacitinib powder, selective JAK1 inhibitor, JAK-STAT pathway regulator, autoimmune inflammation research biochemical raw material

Upadacitinib ABT‑494 Rinvoq CAS 1310726‑60‑3 High‑Purity Powder Selective JAK1 Inhibitor JAK‑STAT Pathway Immunology Biochemical Reagent

High‑purity Upadacitinib powder CAS 1310726‑60‑4, also named ABT‑494 and Rinvoq, is a reversible, orally‑active highly‑selective JAK1 (Janus kinase‑1) small‑molecule inhibitor, with IC50 of 43 nM against JAK1 and around 74‑fold selectivity over JAK2. This off‑white crystalline compound suppresses the JAK‑STAT signalling cascade, cuts down the phosphorylation of STAT protein and inhibits the secretion of multiple pro‑inflammatory cytokines including IL‑6, IFN‑γ and IL‑2. It regulates T‑lymphocyte and regulatory T‑cell balance and relieves chronic immune‑mediated inflammation. Widely utilised for laboratory‑scale research on rheumatoid arthritis, psoriatic arthritis, atopic dermatitis, ulcerative colitis, ankylosing spondylitis and autoimmune‑disease targeted‑drug‑screening projects. Every‑batch undergoes strict HPLC purity inspection, bulk‑order service and customizable‑packaging are available for global immunology and inflammatory‑pharmacology research‑oriented purchasers.

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Upadacitinib (CAS 1310726-60-3) Selective JAK1 Inhibitor | ABT-494 Rinvoq Research Chemical Supplier

Upadacitinib CAS 1310726-60-3
Selective JAK1 Inhibitor (ABT-494)

A next-generation, orally bioavailable selective Janus kinase 1 (JAK1) inhibitor engineered by AbbVie and marketed as Rinvoq. Upadacitinib preferentially blocks JAK1 and JAK1/JAK3 mediated STAT phosphorylation over JAK2/JAK2 signaling, shutting down IL-6, IL-23, IL-4/IL-13 and interferon-gamma driven inflammation. A cornerstone tool compound for rheumatoid arthritis, psoriatic arthritis, psoriasis, atopic dermatitis, ulcerative colitis, Crohn's disease and ankylosing spondylitis research.

Selective JAK1 Inhibitor JAK-STAT Pathway Orally Bioavailable Anti-inflammatory Autoimmune Research ABT-494 / Rinvoq IL-6 & IL-23 Blockade
Request a Quote Technical Specs
380.37
MW (C17H19F3N6O)
≥98%
Purity (HPLC)
JAK1
Selective Target

Molecular Information

Name: Upadacitinib
CAS: 1310726-60-3
Formula: C17H19F3N6O
MW: 380.37 g/mol
Purity: ≥98% (HPLC)
SMILES: CC[C@@H]1CN(C[C@@H]1
  C2=CN=C3N2C4=C(NC=C4)N=C3)
  C(=O)NCC(F)(F)F
InChIKey: WYQFJHHDOKWSHR
  -MNOVXSKESA-N
Appearance: White to off-white powder
Solubility: DMSO (~42 mg/mL)
Synonyms: ABT-494 / Rinvoq
Storage: -20°C, sealed, protect from light
🧪
CAS Number
1310726-60-3
⚖️
Molecular Weight
380.37
🎯
Primary Target
JAK1 Selective
✅
Purity
≥98%

Upadacitinib Technical Specifications & QC Data

Complete physicochemical properties and quality control parameters for research-grade Upadacitinib powder (CAS 1310726-60-3, ABT-494)

📋 Physicochemical Properties

  • Product NameUpadacitinib
  • IUPAC Name(3S,4R)-3-Ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide
  • CAS Number1310726-60-3
  • Code NamesABT-494 / Rinvoq
  • Molecular FormulaC17H19F3N6O
  • Molecular Weight380.37 g/mol
  • Exact Mass380.158 Da
  • SMILESCC[C@@H]1CN(C[C@@H]1C2=CN=C3N2C4=C(NC=C4)N=C3)C(=O)NCC(F)(F)F
  • InChIKeyWYQFJHHDOKWSHR-MNOVXSKESA-N
  • Stereocenters2 defined (3S,4R)
  • AppearanceWhite to off-white crystalline powder
  • LogP / tPSA~3.06 / 78.3 Ų
  • MDL NumberMFCD30502663
  • PubChem CID58557659
  • UNII4RA0KN46E0

🔬 Quality Control & Handling

  • Purity (HPLC)≥98%
  • Chiral Purity(3S,4R) isomer, ee ≥98%
  • FormCrystalline solid / free-flowing powder
  • ColorWhite to off-white
  • Storage Condition-20°C, sealed, dry, protect from light
  • ShippingAmbient with ice pack; cold chain on request
  • SolubilityDMSO ~42 mg/mL; ethanol ~76 mg/mL; DMF ~30 mg/mL; poorly water soluble
  • GHS ClassificationGHS07; H302 (harmful if swallowed)
  • QC DocumentationCOA / HPLC / NMR / MS / MSDS
  • Pack Sizes1g / 5g / 10g / 100g / 1KG
  • Stock StatusIn Stock
  • Use StatementResearch use only; not for human/clinical use

Molecular Targets & JAK Family Selectivity Profile

Upadacitinib was rationally designed for JAK1 selectivity — inhibiting JAK1 and JAK1/JAK3 heterodimer signaling far more potently than JAK2 homodimer signaling that governs erythropoiesis

🎯 JAK1 (Primary Target) 🔗 JAK1/JAK3 Heterodimer 🔗 JAK1/TYK2 Heterodimer ⬇️ JAK2/JAK2 (Spared) 🧬 STAT1 / STAT3 / STAT5 🔥 IL-6 / gp130 Axis 🦠 IL-23 / Th17 Axis 🌡️ IFN-γ Signaling 🧫 IL-4 / IL-13 (Th2) ⚡ IL-2 / IL-7 / IL-15 / IL-21 🛡️ Type I Interferons 🧠 IL-12 / Th1 Polarization

How Upadacitinib Works: Selective JAK1 Blockade of the JAK-STAT Pathway

A stepwise view of how ATP-competitive JAK1 inhibition translates into broad, multi-cytokine anti-inflammatory activity

1

Cytokine Receptor Engagement

Pro-inflammatory cytokines (IL-6, IL-23, IL-12, IFN-γ, IL-4/IL-13, common γ-chain cytokines) bind their type I/II receptors, driving receptor dimerization and juxtaposition of receptor-associated Janus kinases.

2

ATP-Competitive JAK1 Inhibition

Upadacitinib occupies the ATP-binding cleft of the JAK1 kinase domain. Its (3S,4R)-pyrrolidine carboxamide scaffold exploits subtle hinge-region differences to achieve functional selectivity for JAK1 over JAK2.

3

Loss of STAT Phosphorylation

Without active JAK1, receptor tyrosines are not phosphorylated, STAT1/STAT3/STAT5 recruitment fails, and phospho-STAT dimers cannot form — the key measurable readout in leukocyte pSTAT assays.

4

Blocked Nuclear Transcription

STAT dimers never translocate to the nucleus, so transcription of inflammatory gene programs (acute-phase proteins, chemokines, matrix metalloproteinases, RANKL) is suppressed at source.

5

Multi-Axis Immune Modulation

Because JAK1 is shared by Th1, Th2 and Th17 cytokine receptors, a single JAK1-selective agent dampens all three inflammatory axes simultaneously — the pharmacological basis for its breadth across autoimmune indications.

6

JAK2 Sparing Rationale

Erythropoietin and thrombopoietin signal through JAK2 homodimers. Relative JAK2 sparing is the design rationale intended to limit hematologic effects seen with less selective pan-JAK inhibitors.

Research Applications & Disease Models for Upadacitinib

From rheumatology to dermatology and gastroenterology — where a selective JAK1 inhibitor is the tool compound of choice

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Rheumatoid Arthritis Research

The flagship indication. Used in collagen-induced arthritis and adjuvant arthritis models to probe IL-6/STAT3-driven synovitis, osteoclastogenesis via RANKL, pannus formation and cartilage degradation. Upadacitinib was FDA-approved for moderate-to-severe active RA in August 2019.

FDA Approved 2019
🩹

Psoriasis & Psoriatic Arthritis

JAK1-dependent IL-23/IL-22 signaling drives keratinocyte hyperproliferation and Th17 skin inflammation. Applied in imiquimod-induced psoriasiform dermatitis models, enthesitis studies and dactylitis endpoints relevant to psoriatic arthritis pathology.

Th17 / IL-23 Axis
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Atopic Dermatitis & Itch Biology

IL-4, IL-13 and IL-31 all signal through JAK1, making selective JAK1 inhibition a powerful probe for type-2 skin inflammation and pruritus. Common readouts include EASI-equivalent lesion scoring, scratching behavior, filaggrin expression and skin barrier TEWL in mouse models.

Type 2 Inflammation
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Ulcerative Colitis & Crohn's Disease

Used in DSS-colitis, TNBS-colitis and T-cell transfer IBD models to interrogate mucosal healing, epithelial barrier integrity, colonic pSTAT3 and fecal calprotectin. Upadacitinib is approved for both ulcerative colitis and Crohn's disease in human medicine.

IBD Research
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Ankylosing Spondylitis & Axial SpA

A reference agent for axial spondyloarthritis studies covering sacroiliac joint inflammation, new bone formation, spinal MRI inflammation scores and the IL-23/IL-17 to JAK1 signaling interface in enthesis-resident immune cells.

Spondyloarthritis
⚙️

JAK-STAT Signaling Mechanism Studies

A benchmark chemical probe for dissecting JAK isoform contributions. Standard workflows include phospho-flow pSTAT1/3/5 profiling in whole blood, kinome selectivity panels, cytokine-stimulated PBMC assays and CRISPR JAK1-knockout comparisons.

Chemical Probe
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Autoimmune & Interferonopathy Models

Applied in systemic lupus erythematosus, Sjögren's syndrome, dermatomyositis and type I interferonopathy research where JAK1/TYK2-driven interferon signatures dominate. Useful for evaluating interferon-stimulated gene (ISG) score suppression.

Interferon Signature
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Alopecia Areata & Vitiligo

IFN-γ/CXCL10 mediated collapse of hair-follicle and melanocyte immune privilege is JAK1/JAK2 dependent. Selective JAK1 inhibitors are studied for hair regrowth (SALT score analogues) and repigmentation endpoints in preclinical dermatology models.

Dermatology
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ADME, DMPK & Analytical Reference

Used as an analytical reference standard for LC-MS/MS bioanalysis, CYP3A4/CYP2D6 metabolism studies, acyl glucuronide (M4) metabolite identification, protein-binding determination and extended-release formulation development.

Reference Standard

Key Publications & Landmark Clinical Literature

Pivotal papers documenting the discovery, JAK1 selectivity and clinical evaluation of upadacitinib (ABT-494)

Burmester GR, Kremer JM, Van den Bosch F, et al. Safety and efficacy of upadacitinib in patients with rheumatoid arthritis and inadequate response to conventional synthetic disease-modifying anti-rheumatic drugs (SELECT-NEXT): a randomised, double-blind, placebo-controlled phase 3 trial. The Lancet. 2018;391(10139):2503-2512.
doi: 10.1016/S0140-6736(18)31115-2
Genovese MC, Fleischmann R, Combe B, et al. Safety and efficacy of upadacitinib in patients with active rheumatoid arthritis refractory to biologic DMARDs (SELECT-BEYOND): a double-blind, randomised controlled phase 3 trial. The Lancet. 2018;391(10139):2513-2524.
doi: 10.1016/S0140-6736(18)31116-4
Rubbert-Roth A, Enejosa J, Pangan AL, et al. Trial of upadacitinib or abatacept in rheumatoid arthritis (SELECT-CHOICE). New England Journal of Medicine. 2020;383(16):1511-1521.
doi: 10.1056/NEJMoa2008250
Fleischmann R, Pangan AL, Song IH, et al. Upadacitinib versus placebo or adalimumab in patients with rheumatoid arthritis and an inadequate response to methotrexate (SELECT-COMPARE): a phase 3, double-blind, randomized controlled trial. Arthritis & Rheumatology. 2019;71(11):1788-1800.
doi: 10.1002/art.41032
Parmentier JM, Voss J, Graff C, et al. In vitro and in vivo characterization of the JAK1 selectivity of upadacitinib (ABT-494). BMC Rheumatology. 2018;2:23.
doi: 10.1186/s41927-018-0031-x
Guttman-Yassky E, Teixeira HD, Simpson EL, et al. Once-daily upadacitinib versus placebo in adolescents and adults with moderate-to-severe atopic dermatitis (Measure Up 1 and Measure Up 2): results from two replicate double-blind, randomised controlled phase 3 trials. The Lancet. 2021;397(10290):2151-2168.
doi: 10.1016/S0140-6736(21)00588-2

Upadacitinib Pack Sizes & Ordering Information

Research-grade Upadacitinib powder (CAS 1310726-60-3) available in 1g / 5g / 10g / 100g / 1KG with full QC documentation and bulk custom synthesis support

TierPack SizeStock StatusSuitable ForLead Time & Shipping
Standard1 gIn StockCell-based pSTAT assays, kinase profiling, method developmentSame/next-day ship; ambient with ice pack
Medium5 gIn StockRodent arthritis and colitis pharmacology, dose-ranging studiesSame/next-day ship; express courier
Large10 gIn StockMulti-arm in vivo programs, multi-lab collaborations, HTS librariesSame/next-day ship; DHL/FedEx/UPS
Bulk100 gIn StockFormulation and process development, toxicology batches, scale-upQuote to confirm; double-bagged HDPE drum
Industrial1 KGMade to orderPilot/production scale, CMO supply, long-term supply agreementsScheduled batch delivery; palletized air/sea freight

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

Upadacitinib FAQ — Frequently Asked Questions

What is Upadacitinib (CAS 1310726-60-3) and what is it used for?
Upadacitinib, development code ABT-494 and brand name Rinvoq, is an orally bioavailable small-molecule selective Janus kinase 1 (JAK1) inhibitor discovered by AbbVie. Its molecular formula is C17H19F3N6O with a molecular weight of 380.37 g/mol. In research settings it is used to interrogate JAK-STAT signaling and as a positive control in models of rheumatoid arthritis, psoriatic arthritis, atopic dermatitis, ulcerative colitis, Crohn's disease and ankylosing spondylitis.
How is Upadacitinib different from tofacitinib? Is it really JAK1 selective?
Yes — selectivity is the defining feature. Tofacitinib is a pan-JAK inhibitor with potent JAK1/JAK3 plus meaningful JAK2 activity; baricitinib targets JAK1 and JAK2. Upadacitinib was optimized so that in human leukocyte cellular assays it inhibits JAK1 and JAK1/JAK3 mediated STAT phosphorylation more potently than JAK2/JAK2 mediated signaling (Parmentier et al., BMC Rheumatol 2018). Because erythropoietin and thrombopoietin signal through JAK2 homodimers, sparing JAK2 is the rationale for reducing hematologic liabilities while retaining anti-inflammatory potency.
What exactly is the JAK-STAT pathway that Upadacitinib blocks?
The JAK-STAT pathway is the principal intracellular relay for more than 50 cytokines. A cytokine binds its receptor → receptor-associated Janus kinases (JAK1, JAK2, JAK3, TYK2) trans-phosphorylate each other and the receptor tail → STAT proteins dock via SH2 domains and are phosphorylated → phospho-STAT dimers translocate to the nucleus and switch on inflammatory transcription. Upadacitinib is ATP-competitive at the JAK1 kinase domain, so the cascade stops at the very first step.
Which cytokines are affected by selective JAK1 inhibition?
JAK1 partners with JAK2, JAK3 or TYK2 across a very wide receptor set: the IL-6 family via gp130, IL-23 and IL-12, the common γ-chain cytokines IL-2, IL-4, IL-7, IL-9, IL-15 and IL-21, IL-13 and IL-31, plus type I interferons and IFN-γ. This is why one JAK1-selective molecule can suppress Th1, Th2 and Th17 inflammation at once — a pharmacological breadth that biologics targeting a single cytokine cannot match.
Why do JAK inhibitors carry a boxed warning?
The JAK inhibitor class carries a boxed warning for serious infections (including tuberculosis and herpes zoster reactivation), mortality, malignancy including lymphoma, major adverse cardiovascular events (MACE) and thrombosis. The warning derives largely from the ORAL Surveillance post-marketing safety study of tofacitinib and was applied across the class. This is scientific context only — the material supplied here is strictly for laboratory research use and must not be administered to humans or animals for therapeutic purposes.
Is Upadacitinib used for inflammatory bowel disease (IBD) research?
Yes, extensively. JAK1-dependent IL-6, IL-23 and interferon signaling drives mucosal T-cell activation and epithelial barrier breakdown in ulcerative colitis and Crohn's disease. Typical preclinical designs use DSS-induced colitis, TNBS colitis or naive T-cell transfer models with endpoints including disease activity index, colon length, histologic remission, colonic phospho-STAT3 and fecal calprotectin. Upadacitinib is approved in human medicine for both ulcerative colitis and Crohn's disease.
How should Upadacitinib powder be dissolved and stored?
Upadacitinib is readily soluble in DMSO (~42 mg/mL), ethanol (~76 mg/mL) and DMF (~30 mg/mL), with low aqueous solubility. Prepare a concentrated DMSO master stock, aliquot into single-use vials to avoid freeze-thaw degradation, and store at -20°C or -80°C protected from light. Keep final DMSO ≤0.1% v/v in cell culture. For in vivo dosing, common vehicles include DMSO/PEG300/Tween-80/saline or 0.5% methylcellulose suspensions. Store the solid powder sealed and dry at -20°C.
What is the stereochemistry of Upadacitinib and why does it matter?
Upadacitinib is the single enantiomer (3S,4R) of a 3-ethyl-4-(imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)pyrrolidine-1-carboxamide. The two defined stereocenters position the ethyl group and the tricyclic hinge-binding heteroaromatic precisely within the JAK1 ATP pocket. The opposite enantiomer and the diastereomers are markedly less potent, so chiral purity is a critical quality attribute — our COA reports enantiomeric excess alongside HPLC purity.
Do you provide a COA, NMR and mass spec data for each lot?
Yes. Every batch of upadacitinib ships with a Certificate of Analysis (COA) that includes the HPLC purity chromatogram, 1H NMR structural confirmation, LC-MS identity, appearance, water content and residual solvent data. MSDS/SDS, chiral HPLC traces, solubility datasheets and Certificates of Origin are available on request for regulatory or grant documentation.
What pack sizes are available and can you supply bulk kilogram quantities?
Catalog pack sizes are 1 g, 5 g, 10 g, 100 g and 1 KG. The 1 g through 100 g tiers are held in stock for immediate dispatch; the 1 KG industrial tier is made to order with scheduled batch delivery. Custom intermediate quantities, repeat-supply agreements and tiered bulk pricing are supported — contact our team with your target quantity and timeline.

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Research-grade Upadacitinib / ABT-494 powder — purity ≥98% HPLC, COA included, 1g to 1KG
The benchmark selective JAK1 inhibitor for autoimmune, dermatology and IBD research — request a quote today

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Weight 1 g

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