2-Propenamide, N-[5-[[4-[[5-chloro-4-fluoro-2-(1-hydroxy-1-methylethyl)phenyl]amino]-2-pyrimidinyl]amino]-2-[(3S)-3-(dimethylamino)-1-pyrrolidinyl]-4-methoxyphenyl]-
- Product Name
- 2-Propenamide, N-[5-[[4-[[5-chloro-4-fluoro-2-(1-hydroxy-1-methylethyl)phenyl]amino]-2-pyrimidinyl]amino]-2-[(3S)-3-(dimethylamino)-1-pyrrolidinyl]-4-methoxyphenyl]-
- CAS No.
- 2370013-49-1
- Chemical Name
- 2-Propenamide, N-[5-[[4-[[5-chloro-4-fluoro-2-(1-hydroxy-1-methylethyl)phenyl]amino]-2-pyrimidinyl]amino]-2-[(3S)-3-(dimethylamino)-1-pyrrolidinyl]-4-methoxyphenyl]-
- Synonyms
- DZD9008;Shuvotinib;(S)-DZD9008;dzd9008 DZD-9008;(S)-Sunvozertinib;DZD9008vozertinib;Zolotinib AZD3759;Shuvotinib DZD9008;Sunvozertinib (DZD9008);(S)-Sunvozertinib ((S)-DZD9008)
- CBNumber
- CB59270766
- Molecular Formula
- C29H35ClFN7O3
- Formula Weight
- 584.08
- MOL File
- 2370013-49-1.mol
2-Propenamide, N-[5-[[4-[[5-chloro-4-fluoro-2-(1-hydroxy-1-methylethyl)phenyl]amino]-2-pyrimidinyl]amino]-2-[(3S)-3-(dimethylamino)-1-pyrrolidinyl]-4-methoxyphenyl]- Property
- Density
- 1.35±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : 50 mg/mL (85.60 mM; Need ultrasonic)
- pka
- 12.29±0.70(Predicted)
- form
- Solid
- color
- White to off-white
- InChIKey
- BTMKEDDEMKKSEF-KRWDZBQOSA-N
- SMILES
- C(NC1=CC(NC2=NC=CC(NC3=CC(Cl)=C(F)C=C3C(O)(C)C)=N2)=C(OC)C=C1N1CC[C@H](N(C)C)C1)(=O)C=C
2-Propenamide, N-[5-[[4-[[5-chloro-4-fluoro-2-(1-hydroxy-1-methylethyl)phenyl]amino]-2-pyrimidinyl]amino]-2-[(3S)-3-(dimethylamino)-1-pyrrolidinyl]-4-methoxyphenyl]- Chemical Properties,Usage,Production
Uses
(S)-Sunvozertinib ((S)-DZD9008), the S-enantiomer of Sunvozertinib, shows inhibitory activity against EGFR exon 20 NPH and ASV insertions, EGFR L858R/T790M mutation and Her2 exon20 YVMA insertion (IC50=51.2 nM, 51.9 nM, 1 nM, and 21.2 nM, respectively). (S)-Sunvozertinib also inhibits BTK[1].
Biological Activity
(S)-Sunvozertinib ((S)-DZD9008), the S-enantiomer of Sunvozertinib, shows inhibitory activity against EGFR exon 20 NPH and ASV insertions, EGFR L858R/T790M mutation and Her2 exon20 YVMA insertion (IC50=51.2 nM, 51.9 nM, 1 nM, and 21.2 nM, respectively). (S)-Sunvozertinib also inhibits BTK[1]. (S)-Sunvozertinib shows proliferation inhibition of Ba/F3 EGFR NPH ins (GI50=139.7 nM), Ba/F3 FGFR ASV ins (155.7 nM), NCI-HI975 EGFRL858R/T790M (24.4), Her2 YVMA ins (827 nM) and WT EGFR (84.8 nM)[1].(S)-Sunvozertinib shows proliferation inhibition of BTK WT cells (OCI-LY-10, TMD-8, Ri-1and DB, with GI50 ranging from 13.7-48 nM)[1].
IC 50
EGFR exon 20 NPH: 51.2 nM (IC50); EGFR exon 20 ASV insertion: 51.9 nM (IC50); EGFRL858R/T790M: 1 nM (IC50); Her2 exon 20 YVMA insertion: 21.2 nM (IC50)
References
[1]. Zhengtao LI, et al. Erbb/btk inhibitors. WO2019149164A1.
2-Propenamide, N-[5-[[4-[[5-chloro-4-fluoro-2-(1-hydroxy-1-methylethyl)phenyl]amino]-2-pyrimidinyl]amino]-2-[(3S)-3-(dimethylamino)-1-pyrrolidinyl]-4-methoxyphenyl]- Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from 2-Propenamide, N-[5-[[4-[[5-chloro-4-fluoro-2-(1-hydroxy-1-methylethyl)phenyl]amino]-2-pyrimidinyl]amino]-2-[(3S)-3-(dimethylamino)-1-pyrrolidinyl]-4-methoxyphenyl]- manufacturers
- Product
- DZD9008;Sunvozertinib 2370013-49-1
- Price
- US $0.00-0.00/g
- Min. Order
- 1g
- Purity
- 99% HPLC
- Supply Ability
- 10000
- Release date
- 2024-09-19