SPH5030

• CAT Number: I042928
• CAS Number: 2364326-23-6
• Molecular Formula: C31H31FN8O3
• Molecular Weight: 582.63
• Purity: ≥95%
• Synonyms: (Z)-N-[7-ethoxy-4-[3-methyl-4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)anilino]quinazolin-6-yl]-2-fluoro-3-[(2R)-1-methylpyrrolidin-2-yl]prop-2-enamide
• InChI: InChI=1S/C31H31FN8O3/c1-4-42-28-16-25-23(15-26(28)38-31(41)24(32)13-21-6-5-10-39(21)3)30(35-17-33-25)37-20-7-8-27(19(2)12-20)43-22-9-11-40-29(14-22)34-18-36-40/h7-9,11-18,21H,4-6,10H2,1-3H3,(H,38,41)(H,33,35,37)/b24-13-/t21-/m1/s1
• InChIKey: HTAMCULFUCGZAM-FKYOTISTSA-N
• SMILES: CCOC1=C(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)OC4=CC5=NC=NN5C=C4)C)NC(=O)C(=CC6CCCN6C)F

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].
SPH5030 (0-10 μM; 72 h) shows anti-proliferation activities against tumor cell lines[1].
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].

MiceIV 3 mg/kg
MicePO 10 mg/kg
RatsIV 3 mg/kg
RatsPO 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

Reference

[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.
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