产品
编 号：F753793
分子式：C32H41BrN9O2P
分子量：694.6
分子式：C32H41BrN9O2P
分子量：694.6
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CAS No: 2568086-81-5
产品详情
生物活性：
EGFR-IN-82 (Cmpound 8a) is a potent and orally active EGFR inhibitor with IC50 values of 0.09 and 0.06 nM for EGFRL858R/T790M/C797S and EGFRDel19/T790M/C797S, respectively. EGFR-IN-82 has no significant effect on EGFRWT. EGFR-IN-82 has anti-proliferative activity and inhibits tumor formation in nude mice. EGFR-IN-82 can be used in non-small cell lung cancer research .
体内研究：
EGFR-IN-82 (compound 8a) 体内药代动力学性能优于 Brigatinib (HY-12857)。EGFR-IN-82 (15 - 30 mg/kg, 口服, 14 - 21 天) 中度抑制 PC9-EGFRDel19/T790M/C797S 异种移植小鼠模型肿瘤的生长，高度抑制 Ba/F3-EGFRDel19/T790M/C797S 异种移植小鼠模型肿瘤的生长。在 Balb/C 小鼠中的药代动力学分析RouteDose (mg/kg)Cmax (ng/mL)AUC0-t (ng/mL*h)AUC0-∞(ng/mL*h)t1/2 (h)MRT (h)
p.0.5157415375156323.56Animal Model:PC9-EGFRDel19/T790M/C797S xenograft mice model Ba/F3-EGFR Del19/T790M/C797Sxenograft mice model
Dosage:15 or 30 mg/kg/day, 14-21 days
Administration:Oral gavage (p.o.)
Result:Exhibited moderate inhibition on tumor growth, with a tumor growth inhibition rate (TGI) of 21.60% at 15 mg/kg and 46.79% at 30 mg/kg in PC9-EGFR Del19/T790M/C797Sxenograft mice model. Presented a very strong tumor growth inhibition effect with the TGI of 48.43% at low dose(15 mg/kg) and 82.60% at high dose(30 mg/kg) in xenograft mice model of Ba/F3-EGFR Del19/T790M/C797S.
体外研究：
EGFR-IN-82 (compound 8a) (72 h) 显著抑制 Ba/F3-EGFRDel19/T790M/C797S 细胞的生长，其 IC50 值为 12.7 nM，但对 A431 细胞的生长无显著作用。
EGFR-IN-82 (Cmpound 8a) is a potent and orally active EGFR inhibitor with IC50 values of 0.09 and 0.06 nM for EGFRL858R/T790M/C797S and EGFRDel19/T790M/C797S, respectively. EGFR-IN-82 has no significant effect on EGFRWT. EGFR-IN-82 has anti-proliferative activity and inhibits tumor formation in nude mice. EGFR-IN-82 can be used in non-small cell lung cancer research .
体内研究：
EGFR-IN-82 (compound 8a) 体内药代动力学性能优于 Brigatinib (HY-12857)。EGFR-IN-82 (15 - 30 mg/kg, 口服, 14 - 21 天) 中度抑制 PC9-EGFRDel19/T790M/C797S 异种移植小鼠模型肿瘤的生长，高度抑制 Ba/F3-EGFRDel19/T790M/C797S 异种移植小鼠模型肿瘤的生长。在 Balb/C 小鼠中的药代动力学分析RouteDose (mg/kg)Cmax (ng/mL)AUC0-t (ng/mL*h)AUC0-∞(ng/mL*h)t1/2 (h)MRT (h)
p.0.5157415375156323.56Animal Model:PC9-EGFRDel19/T790M/C797S xenograft mice model Ba/F3-EGFR Del19/T790M/C797Sxenograft mice model
Dosage:15 or 30 mg/kg/day, 14-21 days
Administration:Oral gavage (p.o.)
Result:Exhibited moderate inhibition on tumor growth, with a tumor growth inhibition rate (TGI) of 21.60% at 15 mg/kg and 46.79% at 30 mg/kg in PC9-EGFR Del19/T790M/C797Sxenograft mice model. Presented a very strong tumor growth inhibition effect with the TGI of 48.43% at low dose(15 mg/kg) and 82.60% at high dose(30 mg/kg) in xenograft mice model of Ba/F3-EGFR Del19/T790M/C797S.
体外研究：
EGFR-IN-82 (compound 8a) (72 h) 显著抑制 Ba/F3-EGFRDel19/T790M/C797S 细胞的生长，其 IC50 值为 12.7 nM，但对 A431 细胞的生长无显著作用。
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