product Description
Upadacitinib (Crystal Form C) (CAS No.: 1310726-60-3; molecular formula: C₁₇H₁₉F₃N₆O; molecular weight: 380.37) is a highly selective Janus kinase 1 (JAK1) inhibitor, serving as a core bulk pharmaceutical raw material for the research and production of anti-inflammatory and autoimmune disease therapeutic drugs. It features specific crystal form characteristics and stable physicochemical properties, with excellent solubility in organic solvents and strict quality control indicators, making it a key raw material in the pharmaceutical field for the preparation of targeted therapeutic formulations.
As a high-purity bulk pharmaceutical chemical, Upadacitinib (Crystal Form C) is presented as white or off-white to light yellow to grayish-brown to light brown powder or solid, with the characteristic of organic fluoride compound. It is freely soluble in anhydrous ethanol, slightly soluble in acetonitrile and ethyl acetate, and almost insoluble in water. The stable crystal form structure ensures the consistency of its physicochemical properties and drug efficacy, and it must be stored in a sealed and dry environment protected from light to maintain the stability of the crystal form and prevent quality degradation.
For quality control, Upadacitinib (Crystal Form C) complies with strict in-house specifications of pharmaceutical grade: the assay is 98.0%~102.0% (calculated on dried substance); the control of related substances is stringent with specified single impurity WPT-IMP45 not detected, other individual impurities ≤0.10% and total impurities ≤1.0%; key isomers WPT-IMP6, WPT-IMP12 and WPT-IMP19 are all not detected (≤0.1%). It also strictly controls residual solvents, chlorides, sulfates, heavy metals, moisture and residue on ignition to ensure the high purity and safety of the bulk drug, meeting the quality requirements for pharmaceutical production and batch consistency.
Pharmaceutically, Upadacitinib (Crystal Form C) is the core raw material for the synthesis of JAK1 inhibitor targeted drugs, which is widely used in the research and development and production of therapeutic drugs for various immune-mediated inflammatory diseases. It exerts anti-inflammatory and immune-regulatory effects by selectively inhibiting the JAK1 signaling pathway to interfere with cytokine transmission, and is the key bulk drug for the preparation of formulations for the treatment of atopic dermatitis, rheumatoid arthritis, psoriatic arthritis, ulcerative colitis and other diseases, with important application value in the field of anti-rheumatic and dermatological targeted therapy.
As a high-purity pharmaceutical raw material, Upadacitinib (Crystal Form C) needs to be operated in accordance with the pharmaceutical production specifications: avoid direct contact with skin and mucous membranes during operation, wear appropriate protective equipment, and strictly follow the sealed storage requirements to prevent contamination and crystal form transformation. The transportation and storage must comply with the pharmaceutical raw material management specifications to ensure the quality stability and safety of the product during the circulation process.
Test Items and Results Production Information
|
Test items |
Specifications |
Results |
Judgment |
|
Appearance |
White or off-white to light yellow to grayish-brown to light brown powder or solid |
Light brown powder |
Conforms |
|
Solubility |
Freely soluble in anhydrous ethanol, slightly soluble in acetonitrile, slightly soluble in ethyl acetate, and almost insoluble in water |
Conform to standard |
Conforms |
|
Identification |
Chemical identification: Identification reaction of apparent organic fluorides; Infrared absorption spectra should be consistent with the reference spectra |
Conform to standard |
Conforms |
|
Related substance - WPT-IMP45 (%) |
≤0.1 |
Not detected |
Conforms |
|
Related substance - Other individual impurities (%) |
≤0.10 |
0.02 |
Conforms |
|
Related substance - Total Impurity (%) |
≤1.0 |
0.05 |
Conforms |
|
Isomer - WPT-IMP6 (%) |
≤0.1 |
Not detected |
Conforms |
|
Isomer - WPT-IMP12 (%) |
<0.1 |
Not detected |
Conforms |
|
Isomer - WPT-IMP19 (%) |
≤0.1 |
Not detected |
Conforms |
|
Residual solvents - Ethyl alcohol (%) |
≤0.5 |
0.04 |
Conforms |
|
Residual solvents - Acetonitrile (%) |
≤0.041 |
Not detected |
Conforms |
|
Residual solvents - Ethyl acetate (%) |
≤0.5 |
0.16 |
Conforms |
|
Residual solvents - N-heptane (%) |
≤0.5 |
0.01 |
Conforms |
|
Chlorides (%) |
≤0.04 |
<0.04 |
Conforms |
|
Sulfate (%) |
≤0.04 |
<0.04 |
Conforms |
|
Heavy metals |
Not more than ten parts per million |
Less than one in a million |
Conforms |
|
Moisture (%) |
2.0~3.0 |
2.25 |
Conforms |
|
Residue on ignition (%) |
≤0.1 |
0.03 |
Conforms |
|
Assay (dried substance, %) |
98.0%~102.0% |
101.3 |
Conforms |
|
Conclusion |
- |
- |
Comply with the in-house specification |
Storage and Transport Conditions
Transport Conditions: Keep sealed and dry during transportation, protect from light, avoid violent collision and ensure the integrity of packaging.Storage Conditions: Keep sealed in dry container, protect from light at room temperature, avoid damp and contamination, and the validity period is subject to the marked date on the product label.
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