GZD856 formic
Based on 1 Customer Validation
GZD856 formic is a potent and orally active PDGFRα/β inhibitor, with IC50s of 68.6 and 136.6 nM, respectively. GZD856 formic is also a Bcr-AblT315I inhibitor, with IC50s of 19.9 and 15.4 nM for native Bcr-Abl and the T315I mutant. GZD856 formic has antitumor activity. GZD856 (formic) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- Purity: 95.36%
- CAS No.: 2804039-78-7
- 화학식: C30H29F3N6O3
- 분자량:578.58
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보관:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
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PDGFRα 68.6 nM (IC50) |
PDGFRβ 136.6 nM (IC50) |
Bcr-AblT315I 15.4 nM (IC50) |
Bcr-Abl 19.9 nM (IC50) |
GZD856 (0.0032-10 μM, 72 h) exerts antiproliferative activity against a panel of lung cancer cells[1].
GZD856 (0.3-3 μM; 24-28 h) induces a dose-dependent G0/G1 phase arrest and apoptosis in H1703 but not A549 cells[1].
GZD856 (0.1-10 μM; 6 h) dose-dependently inhibits the PDGFRα/β phosphorylation and downstream signaling in H1703 and A549 cells[1].
GZD856 inhibits 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H1703, A549, Calu-6, 95-D, L-78, HCC827, SPCA-1, H1650, H1299, H522, H332 and H820 NSCLC cells
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Concentration:0.0032-10 μM
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Incubation Time:72 hours
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Result:Inhibited PDGFRα-overexpressing H1703 cells, with an IC50 of 0.25 μM.
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Cell Line:H1703 and A549 NSCLC cells
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Concentration:0.3, 1, 3 μM
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Incubation Time:24, 48 hours
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Result:Led to 54.1% apoptosis in H1703 cells at the concentration of 3.0 µM, whereas only 15.5% apoptotic A549 cells were observed under similar conditions.
Decreased the CDK4, cyclin D2, CDK2 and Cyclin E protein levels and activated of PARP and Caspase-3 cleavage in H1703 cells.
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Cell Line:H1703 and A549 NSCLC cells
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Concentration:0.1-10 μM
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Incubation Time:6 hours
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Result:Inhibited the phosphorylation of PDGFRα and PDGFRβ in a dose-dependent manner.
Observed the activation of downstream AKT, ERK1/2 and STAT3, with no obvious effects on total protein levels.
GZD856 (10 mg/kg; p.o. once daily for 8 d) potently inhibits tumor growth in mouse bearing xenograft K562 and Ba/F3 cells expressing Bcr-AblT315I[2].
GZD856 (5 mg/kg; a single i.v.) exhibits a long half-life (T1/2=19.97 h), optimal plasma exposure (Cmax=934.38 μg/L) and a AUC0-∞ (8165.8 μg/L h) in rats[1].
GZD856 (25 mg/kg; a single p.o.) exhibits a long half-life (T1/2=22.2 h), optimal plasma exposure (Cmax=899.5 μg/L) and a good oral bioavailability (BA=78%) in rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male CB17-SCID mice implanted with H1703 and A549 cancer cells[1]
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Dosage:10, 30 mg/kg
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Administration:Oral gavage once daily for 16 days
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Result:Displayed antitumor effects in H1703-xenograft mice, with tumor growth inhibition (TGI) values of 20.8% and 74.1% at dosages of 10 and 30 mg/kg, respectively.
Displayed antitumor effects in A549-xenograft mice, with a TGI value of 51.1% at 30 mg/kg.
Was well tolerated in all of the tested groups, with no mortality or significant loss of body weight.
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Animal Model:Sprague-Dawley (SD) rats (180-220 g)[1]
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Dosage:5 mg/kg for i.v.; 25 mg/kg for p.o. (Pharmacokinetic Analysis)
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Administration:A single intravenous injection and oral administration
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Result:I.v.: T1/2=19.97 h; Cmax=934.38 μg/L; AUC0-∞=8165.8 µg/L•h.
P.o.: T1/2=22.2 h; Cmax=899.5 μg/L; BA=78%.
Chemical Information
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CAS No. 2804039-78-7
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Appearance Solid
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분자량 578.58
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화학식 C30H29F3N6O3
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Color Off-white to light yellow
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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.OC=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
용액&용해도
DMSO : 100 mg/mL (172.84 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (281 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Zhang Z, et, al. GZD856, a novel potent PDGFRα/β inhibitor, suppresses the growth and migration of lung cancer cells in vitro and in vivo. Cancer Lett. 2016 May 28;375(1):172-178. [Content Brief]
[2]. Lu X, et, al. Synthesis and identification of GZD856 as an orally bioavailable Bcr-Abl T315I inhibitor overcoming acquired imatinib resistance. J Enzyme Inhib Med Chem. 2017 Dec;32(1):331-336. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7284 mL | 8.6418 mL | 17.2837 mL | 43.2092 mL |
| 5 mM | 0.3457 mL | 1.7284 mL | 3.4567 mL | 8.6418 mL | |
| 10 mM | 0.1728 mL | 0.8642 mL | 1.7284 mL | 4.3209 mL | |
| 15 mM | 0.1152 mL | 0.5761 mL | 1.1522 mL | 2.8806 mL | |
| 20 mM | 0.0864 mL | 0.4321 mL | 0.8642 mL | 2.1605 mL | |
| 25 mM | 0.0691 mL | 0.3457 mL | 0.6913 mL | 1.7284 mL | |
| 30 mM | 0.0576 mL | 0.2881 mL | 0.5761 mL | 1.4403 mL | |
| 40 mM | 0.0432 mL | 0.2160 mL | 0.4321 mL | 1.0802 mL | |
| 50 mM | 0.0346 mL | 0.1728 mL | 0.3457 mL | 0.8642 mL | |
| 60 mM | 0.0288 mL | 0.1440 mL | 0.2881 mL | 0.7202 mL | |
| 80 mM | 0.0216 mL | 0.1080 mL | 0.2160 mL | 0.5401 mL | |
| 100 mM | 0.0173 mL | 0.0864 mL | 0.1728 mL | 0.4321 mL |
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