Gusacitinib
- Product Name
- Gusacitinib
- CAS No.
- 1425381-60-7
- Chemical Name
- Gusacitinib
- Synonyms
- ASN-002;GUSACITINIB;GUSACITINIB (ASN-002);ASN-002 (Gusacitinib;Gusacitinib, 10 mM in DMSO;Syk,Janus kinase,Gusacitinib,Spleen tyrosine kinase,JAK,ASN 002,ASN002,Inhibitor,inhibit;1-[5,6-Dihydro-4-[[4-(4-hydroxy-1-piperidinyl)phenyl]amino]-5-oxopyrimido[4,5-d]pyridazin-2-yl]-4-piperidineacetonitrile;4-Piperidineacetonitrile, 1-[5,6-dihydro-4-[[4-(4-hydroxy-1-piperidinyl)phenyl]amino]-5-oxopyrimido[4,5-d]pyridazin-2-yl]-;2-(1-(4-((4-(4-hydroxypiperidin-1-yl)phenyl)amino)-5-oxo-5,6-dihydropyrimido[4,5-d]pyridazin-2-yl)piperidin-4-yl)acetonitrile
- CBNumber
- CB03364604
- Molecular Formula
- C24H28N8O2
- Formula Weight
- 460.53
- MOL File
- 1425381-60-7.mol
Gusacitinib Property
- Density
- 1.47±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO:100.0(Max Conc. mg/mL);217.14(Max Conc. mM)
- form
- A crystalline solid
- pka
- 9.17±0.20(Predicted)
- color
- Light yellow to yellow
- InChI
- InChI=1S/C24H28N8O2/c25-10-5-16-6-11-32(12-7-16)24-28-20-15-26-30-23(34)21(20)22(29-24)27-17-1-3-18(4-2-17)31-13-8-19(33)9-14-31/h1-4,15-16,19,33H,5-9,11-14H2,(H,30,34)(H,27,28,29)
- InChIKey
- NLFLXLJXEIUQDL-UHFFFAOYSA-N
- SMILES
- N1(C2=NC(NC3=CC=C(N4CCC(O)CC4)C=C3)=C3C(=O)NN=CC3=N2)CCC(CC#N)CC1
N-Bromosuccinimide Price
- Product number
- CS-0023113
- Product name
- Gusacitinib
- Purity
- 99.41%
- Packaging
- 25mg
- Price
- $250
- Updated
- 2021/12/16
- Product number
- CS-0023113
- Product name
- Gusacitinib
- Purity
- 99.41%
- Packaging
- 50mg
- Price
- $450
- Updated
- 2021/12/16
- Product number
- CS-0023113
- Product name
- Gusacitinib
- Purity
- 99.41%
- Packaging
- 100mg
- Price
- $750
- Updated
- 2021/12/16
- Product number
- DC21100
- Product name
- Gusacitinib(ASN-002)
- Purity
- >98%
- Packaging
- 250mg
- Price
- $950
- Updated
- 2021/12/16
- Product number
- DC21100
- Product name
- Gusacitinib(ASN-002)
- Purity
- >98%
- Packaging
- 1g
- Price
- $1900
- Updated
- 2021/12/16
Gusacitinib Chemical Properties,Usage,Production
Description
Gusacitinib is an orally bioavailable, potent dual inhibitor of Janus kinases (JAK 1, 2, 3, and TYK2) and spleen tyrosine kinase (SYK) with 50% inhibitory concentrations (IC50 values) of 5 to 46 nM in biochemical assays. Gusacitinib targets both Th1 and Th2 inflammatory pathways, which are involved in CHE[1].
Uses
Gusacitinib is an oral Janus and Spleen tyrosine kinase inhibitor. It has been approved by the FDA for the treatment of moderate to severe chronic hand eczema. Gusacitinib is currently being used in clinical studies for the treatment of low-risk nodular basal cell carcinoma in adults.
brand name
ASN-002, EN-3351
Safety
During part A, 60 (61.9%) patients reported at least 1 AE (40 mg, 19 [57.6%]; 80 mg, 24 [75.0%]; and placebo, 17 [53.1%]). Most events were mild or moderate in severity. The most common events (≥10%) were upper respiratory infection, headache, and nausea with headache and gastrointestinal symptoms which were more prevalent with the 80 mg gusacitinib dose. The most common treatment-related events were headache and nausea. Three placebo patients were discontinued because of worsening of CHE. No serious AEs were considered to be related to the study treatment. Creatine phosphokinase elevations, known as drug class effect, were observed starting at week 4 (active treatment) and at week 20 (part B, placebo patients crossing over to 80 mg). No serious AEs were related to the study treatment. Five patients had creatine phosphokinase elevations reported as AEs. No thromboembolic or major cardiovascular events, malignancies, or deaths occurred[1].
in vitro
Gusacitinib shows anti-proliferative activity in a broad panel of human cancer cell lines, including DHL6, DHL4, OCI-LY10, H929, Pfeiffer, HT-1376, and Lovo, suggesting activity in both solid and hematological tumor types.
in vivo
Gusacitinib exhibits significant efficacy in inhibiting tumor growth (>95%) in a multiple myeloma (H929) xenograft model. Gusacitinib significantly delays the onset of hind limb paralysis in the human erythroleukemia (HEL) mouse model. Gusacitinib shows a favorable safety profile in rat and dog toxicology studies.
References
[1] Pablo A. Jimenez MD . “Oral spleen tyrosine kinase/Janus Kinase inhibitor gusacitinib for the treatment of chronic hand eczema: Results of a randomized phase 2 study.” Journal of the American Academy of Dermatology 89 2 (2023): Pages 235-242.
Gusacitinib Preparation Products And Raw materials
Raw materials
Preparation Products
Gusacitinib Suppliers
- Tel
- 010-88886666-01 13112345678
- Fax
- CDXH21@126.com
- loyson@tcypharm.com
- Country
- China
- ProdList
- 596
- Advantage
- 55
- Tel
- 13816752554
- 1745533547@qq.com
- Country
- China
- ProdList
- 129
- Advantage
- 58
- Tel
- 13720134139 086-15871494362 13720134139
- orders@jknbiochem.com
- Country
- China
- ProdList
- 5968
- Advantage
- 58
- Tel
- 0556-5032306 18917961636
- Fax
- +86-556-5032307
- wtx@bayeebio.com
- Country
- China
- ProdList
- 267
- Advantage
- 61
- Tel
- 28-83379370 13880556291
- Fax
- 028-87747383
- tcy@tcypharm.com
- Country
- China
- ProdList
- 510
- Advantage
- 57
- Tel
- 18149758185 18149758185
- sales-cpd@caerulumpharma.com
- Country
- China
- ProdList
- 3466
- Advantage
- 58
- Tel
- 0512-62857507
- Fax
- +86-512-62857507
- sales@sinorarechem.com
- Country
- China
- ProdList
- 997
- Advantage
- 58
- Tel
- 021-52996696，15000506266 15000506266
- Fax
- +86-21-52996696
- Country
- China
- ProdList
- 4587
- Advantage
- 55
- Tel
- 18122150900
- Fax
- QQ:2869377561
- sculk28@163.com
- Country
- China
- ProdList
- 646
- Advantage
- 55
- Tel
- 021-65675885 18964387627
- Fax
- 021-65675885
- info@efebio.com
- Country
- China
- ProdList
- 9804
- Advantage
- 58
- Tel
- 17754423994 17754423994
- Fax
- QQ:2853530913
- 2853530910@QQ.com
- Country
- China
- ProdList
- 8011
- Advantage
- 62
- Tel
- 21-31433387 15618786686
- Fax
- QQ:1369748377
- sales@rechemscience.com
- Country
- China
- ProdList
- 2991
- Advantage
- 58
- Tel
- 028-83379370 13880556291
- Fax
- 028-87747383
- tcy@tcypharm.com
- Country
- China
- ProdList
- 6274
- Advantage
- 58
- Tel
- 010-50973130 4009686088
- 3193328036@qq.com
- Country
- China
- ProdList
- 29764
- Advantage
- 68
- Tel
- 17317130613
- Fax
- QQ3358272972
- 3358272972@qq.com
- Country
- China
- ProdList
- 3254
- Advantage
- 58
- Tel
- 028-85157043 15882256948
- 676046971@qq.com
- Country
- China
- ProdList
- 4399
- Advantage
- 58
- Tel
- 13880556291
- Fax
- 028-87747383
- fuwei@tcypharm.com
- Country
- China
- ProdList
- 235
- Advantage
- 58
- Tel
- 86-571-88216897,88216896 13588875226
- Fax
- 86-571-88216895
- sales@hzclap.com
- Country
- CHINA
- ProdList
- 6312
- Advantage
- 58
- Tel
- +86-0371-86658258 +8613203830695
- Fax
- 0371-86658258
- laboratory@coreychem.com
- Country
- China
- ProdList
- 30231
- Advantage
- 58
- Tel
- 021-58447131 13564518121
- sales@dcchemicals.com
- Country
- China
- ProdList
- 9409
- Advantage
- 58
- Tel
- 0519-85788828 13775037613
- sales@chemrenpharm.com
- Country
- China
- ProdList
- 3600
- Advantage
- 58
- Tel
- 18818260767
- Fax
- QQ 3610331285
- sales@chemegen.com
- Country
- China
- ProdList
- 11218
- Advantage
- 58
- Tel
- 021-51111890 15317326293
- sales@molnova.com
- Country
- China
- ProdList
- 4195
- Advantage
- 58
- Tel
- 15342225168
- yutianchun2007@126.com
- Country
- China
- ProdList
- 10002
- Advantage
- 58
- Tel
- 13348960310 13348960310
- 3003867561@qq.com
- Country
- China
- ProdList
- 10524
- Advantage
- 58
- Tel
- 021-51816796-820 13611835272
- Fax
- 021-5161 3951
- sales2@sunwaypharm.com
- Country
- China
- ProdList
- 44455
- Advantage
- 58
- Tel
- 14793566
- info@cenpharm.com
- Country
- China
- ProdList
- 752
- Advantage
- 58
- Tel
- 400-1647117 13681763483
- product02@bidepharm.com
- Country
- China
- ProdList
- 62072
- Advantage
- 58
- Tel
- 13549236410
- sales@invivochem.cn
- Country
- China
- ProdList
- 6753
- Advantage
- 58
- Tel
- 13339985473
- C13339985473@163.com
- Country
- China
- ProdList
- 4756
- Advantage
- 58
- Tel
- 512-62857507
- sales@sinorarechem.com
- Country
- China
- ProdList
- 607
- Advantage
- 58
- Tel
- 4008200310
- marketing@tsbiochem.com
- Country
- China
- ProdList
- 24641
- Advantage
- 58
- Tel
- 0371-55013243 15324716602
- 2853979810@qq.com
- Country
- China
- ProdList
- 9940
- Advantage
- 58
- Tel
- 021-57520305 15801958784
- lihua@jskchem.com
- Country
- China
- ProdList
- 49234
- Advantage
- 58
- Tel
- 021-59167510 18117107507
- vip@med-life.cn
- Country
- China
- ProdList
- 4997
- Advantage
- 58
- Tel
- 025-85560043 15850508050
- Fax
- 025-85563444
- cindy.huang@synzest.com
- Country
- China
- ProdList
- 12000
- Advantage
- 58
- Tel
- 400-6206333 1316706386
- anhua.mao@aladdin-e.com
- Country
- China
- ProdList
- 48459
- Advantage
- 58
- Tel
- 17721492509
- 643638326@qq.com
- Country
- China
- ProdList
- 4960
- Advantage
- 58
- Tel
- 13823398779 13823398779
- 184792226@qq.com
- Country
- China
- ProdList
- 3342
- Advantage
- 58
- Tel
- 027-02759101766 13125137661
- 2853877621@qq.com
- Country
- China
- ProdList
- 7450
- Advantage
- 58
- Tel
- 17316404525
- 209533805@qq.com
- Country
- China
- ProdList
- 9970
- Advantage
- 58
- Tel
- 17717618050
- zllg@gh-reagent.com
- Country
- China
- ProdList
- 10422
- Advantage
- 58
- Tel
- 400-821-026
- Sales@sangon.com
- Country
- China
- ProdList
- 47240
- Advantage
- 58
- Tel
- (800)364-9897
- Caymanname@qq.com
- Country
- CHINA
- ProdList
- 21570
- Advantage
- 58
- Tel
- Enzo Biochem Inc.
- Enzoname@qq.com
- Country
- CHINA
- ProdList
- 124556
- Advantage
- 58
- Tel
- +8613720134139
- orders@jknbiochem.com
- Country
- China
- ProdList
- 5221
- Advantage
- 58
- Tel
- +86-852-30606658
- market18@leapchem.com
- Country
- China
- ProdList
- 43340
- Advantage
- 58
- Tel
- --
- Fax
- --
- info@neobioscience.com
- Country
- CHINA
- ProdList
- 6207
- Advantage
- 58
- Tel
- --
- Fax
- --
- chenjw@absin.cn
- Country
- CHINA
- ProdList
- 6025
- Advantage
- 58
- Tel
- --
- Fax
- --
- Proteintech-CN@ptglab.com
- Country
- CHINA
- ProdList
- 6290
- Advantage
- 58