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[바이오클론] [MedChemExpress한국독점대리점] GZD856
바이오클론
Signaling Pathway에 관련된 Biological Inhibitors
와 Biochemical Reagent 제조, 공급하는 회사
인 MedChemExpress(MCE)를 소개합니다.(USA)
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바이오클론(주)는 MedChem Express(MCE)의 한국공식독점대리점이며, 2015년부터 정부의 화학물질의 등록 및 평가 등에 관한 법률(화평법)에 의해 모든 화학물질을 한국환경공단에 신고, 허가 하에 안전하게 수입 공급하고 있습니다.
GZD856
GZD856 화학구조
CAS No. : 1257628-64-0
제품 설명 |
GZD856 is a potent and orally bioavailable PDGFRα/β inhibitor with IC50s of 68.6 and 136.6 nM, respectively.GZD856 is also a Bcr-AblT315I inhibitor with IC50s of 19.9 and 15.4 nM for Bcr-Abl and T315I mutant. Antitumor activity[2]. |
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IC50 & Target[1][2] |
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In Vitro
GZD856 (0.0032-10 μM, 72 h) exerts antiproliferative activity against a panel of lung cancer cells[1].
GZD856 shows dose-dependent inhibition of PDGFRα and PDGFRβ phosphorylation in H1703 and A549 cells, respectively. The activation of downstream AKT (phosphorylation of S473 but not T308), ERK1/2 and STAT3 is also observed after exposure to GZD856, with no obvious effects on total protein levels[1].
GZD856 induces dose-dependent G0/G1 phase arrest and apoptosis in H1703 cells but not in A549 cells[1].
GZD856 strongly suppresses the proliferation of K562, K562R (Q252H) and murine Ba/F3 cells ectopically expressing Bcr-AblWT and Bcr-AblT315I, with IC50s of 2.2, 67.0, 0.64 and 10.8 nM, respectively[2].
Cell Viability Assay[1]
Cell Line: | H1703, A549, Calu-6, 95-D, L-78,HCC827, SPCA-1, H1650, H1299, H522, H332 and H820 NSCLC cells. |
Concentration: | 0.0032-10 μM |
Incubation Time: | 72 h |
Result: | GZD856 displays an IC50 of 0.25 μM against the PDGFRα-overexpressing H1703 cells but is 4–60-fold less potent against PDGFRαnegative human lung cancer cell lines regardless of PDGFRβ expression levels[1]. |
In Vivo
GZD856 (10 and 30 mg/kg/day, 16 days) displays good in vivo antitumor activity in both H1703 and A549 lung cancer models[1].
A 25-mg/kg oral dose of GZD856 exhibits a long half-life of 22.2 h, optimal plasma exposure (Cmax, 899.5 μg/L) and a good oral bioavailability of 78%[1].
GZD856 (10 mg/kg/day, 8 days, oral) potently suppresses tumor growth in mouse bearing xenograft K562 and Ba/F3 cells expressing Bcr-AblT315I[2].
Animal Model: | Male CB17-SCID mice (H1703 and A549 cancer cells)[1] |
Dosage: | 10, 30 mg/kg |
Administration: | Oral gavage,daily,16 consecutive days |
Result: | GZD856 exhibits dose-dependent antitumor efficacy in the xenografted mouse with H1703 cancer cells, with tumor growth inhibition (TGI) values of 20.8% and 74.1% at dosages of 10 and 30 mg/kg/day, respectively. GZD856 also displays obvious in vivo antitumor effects in A549- xenograft mice, with a TGI value of 51.1% at 30 mg/kg[1]. |
분자량
532.56
화학식
C₂₉H₂₇F₃N₆O
CAS No.
1257628-64-0
SMILES
O=C(NC1=CC=C(CN2CCN(C)CC2)C(C(F)(F)F)=C1)C3=CC=C(C)C(C#CC4=CN5C(N=C4)=CC=N5)=C3
선적
Room temperature in continental US; may vary elsewhere.
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
References
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