| Company Name: |
TargetMol Chemicals Inc.
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| Tel: |
15002134094 |
| Email: |
marketing@targetmol.cn |
| Products Intro: |
Product Name:SPH5030
CAS:2364326-23-6
Package:100mg/RMB 24625;50mg/RMB 19420;25mg/RMB 14900
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2-Propenamide, N-[7-ethoxy-4-[[3-methyl-4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)phenyl]amino]-6-quinazolinyl]-2-fluoro-3-[(2R)-1-methyl-2-pyrrolidinyl]-, (2Z)- manufacturers
- SPH5030
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- $3520.00 / 100mg
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2025-10-27
- CAS:2364326-23-6
- Min. Order:
- Purity:
- Supply Ability: 10g
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| | 2-Propenamide, N-[7-ethoxy-4-[[3-methyl-4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)phenyl]amino]-6-quinazolinyl]-2-fluoro-3-[(2R)-1-methyl-2-pyrrolidinyl]-, (2Z)- Basic information |
| Product Name: | 2-Propenamide, N-[7-ethoxy-4-[[3-methyl-4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)phenyl]amino]-6-quinazolinyl]-2-fluoro-3-[(2R)-1-methyl-2-pyrrolidinyl]-, (2Z)- | | Synonyms: | 2-Propenamide, N-[7-ethoxy-4-[[3-methyl-4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)phenyl]amino]-6-quinazolinyl]-2-fluoro-3-[(2R)-1-methyl-2-pyrrolidinyl]-, (2Z)-;SPH5030 | | CAS: | 2364326-23-6 | | MF: | C31H31FN8O3 | | MW: | 582.63 | | EINECS: | | | Product Categories: | | | Mol File: | 2364326-23-6.mol | ![2-Propenamide, N-[7-ethoxy-4-[[3-methyl-4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)phenyl]amino]-6-quinazolinyl]-2-fluoro-3-[(2R)-1-methyl-2-pyrrolidinyl]-, (2Z)- Structure](CAS/20210305/GIF/2364326-23-6.gif) |
| | 2-Propenamide, N-[7-ethoxy-4-[[3-methyl-4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)phenyl]amino]-6-quinazolinyl]-2-fluoro-3-[(2R)-1-methyl-2-pyrrolidinyl]-, (2Z)- Chemical Properties |
| density | 1.38±0.1 g/cm3(Predicted) | | pka | 12.89±0.43(Predicted) | | form | Solid | | color | Off-white to light yellow |
| | 2-Propenamide, N-[7-ethoxy-4-[[3-methyl-4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)phenyl]amino]-6-quinazolinyl]-2-fluoro-3-[(2R)-1-methyl-2-pyrrolidinyl]-, (2Z)- Usage And Synthesis |
| Uses | SPH5030 is a selective and irreversible HER2 inhibitor. SPH5030 inhibits HER2WT and EGFRWT with IC50s of 3.51 and 8.13 nM, respectively. SPH5030 shows excellent activities against HER2 mutants. SPH5030 can be used for the research of cancer[1]. | | in vivo | SPH5030 (5-40 mg/kg; p.o. once per day for 13 or 21 days) shows in vivo antitumor efficacy in mice with xenograft tumor models[1].
1.19 Pharmacokinetic Properties of SPH5030 in Mice and Rats[1]. | Mice
IV 3 mg/kg | Mice
PO 10 mg/kg | Rats
IV 3 mg/kg | Rats
PO 6 mg/kg | | CL (L/kg·h) | 0.70±0.20 | | 0.78±0.13 | | | t1/2 (h) | 3.76±0.15 | 3.60±0.59 | 4.56±0.20 | 4.38±0.35 | | Vss (L/kg) | 2.96±0.96 | | 3.55±0.64 | | | Cmax (μg/mL) | | 1.90±0.14 | | 0.76±0.33 | | tmax (h) | | 2.67±1.15 | | 3.33±1.15 | | AUC0-t (h·μg/mL) | | 13.07±0.48 | | 5.47±2.82 | | F (%) | | 87.66 | | 71.35 |
| Animal Model: | BALB/c nude mouse with NCI-N87 and BT474 xenografts, and NPSG mouse with BAF3 HER2 A775_G776insYVMA xenografts[1] | | Dosage: | 5, 10, 20 and 40 mg/kg | | Administration: | Oral gavage; 5-40 mg/kg once per day; for 13 or 21 days | | Result: | Dose-dependently inhibited tumor growth in NCI-N87, BT474 and BAF3 HER2 A775_G776insYVMA xenograft mouse models, and showed an equivalent or better activity of tumor inhibition compared with neratinib and pyrotinib at a dose of 20 mg/kg. Showed no mortality or significant loss of body weight in xenograft mouse models. |
| | References | [1] Li D,et al. Discovery of SPH5030, a Selective, Potent, and Irreversible Tyrosine Kinase Inhibitor for HER2-Amplified and HER2-Mutant Cancer Treatment. J Med Chem. 2022 Apr 14;65(7):5334-5354. DOI:10.1021/acs.jmedchem.1c00710 |
| | 2-Propenamide, N-[7-ethoxy-4-[[3-methyl-4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)phenyl]amino]-6-quinazolinyl]-2-fluoro-3-[(2R)-1-methyl-2-pyrrolidinyl]-, (2Z)- Preparation Products And Raw materials |
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