Apatinib-d8 free base
Based on 1 Customer Validation
Apatinib-d8 (free base) is the deuterium labeled Apatinib free base. Apatinib free base (YN968D1 free base) is an orally bioavailable tyrosine kinase inhibitor, which selectively targets VEGFR-2 (IC50=1 nM). Apatinib free base (YN968D1 free base) is an anti-angiogenic drug for the research of advanced or metastatic gastric cancer. Apatinib free base (YN968D1 free base) potently inhibits Ret, c-Kit and c-Src with IC50s of 13, 429 and 530 nM, respectively. It also inhibits cellular phosphorylation of VEGFR-2, c-kit and PDGFRβ.
For research use only. We do not sell to patients.
- Purity: 92.03%
- CAS No.: 2468771-43-7
- Formula: C24H15D8N5O
- Molecular Weight:405.52
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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CAS No. 2468771-43-7
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Unlabeled Cas 811803-05-1
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Appearance Solid
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Molecular Weight 405.52
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Formula C24H15D8N5O
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Color Off-white to light yellow
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SMILES
O=C(C1=CC=CN=C1NCC2=CC=NC=C2)NC3=CC=C(C4(C#N)C([2H])([2H])C([2H])([2H])C([2H])([2H])C4([2H])[2H])C=C3
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Synonyms
YN968D1-d8 free base
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 30 mg/mL (73.98 mM; Need ultrasonic and warming; 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)
Purity & Documentation
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Data Sheet (279 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. [Content Brief]
[2]. Roviello G, et al. Apatinib: A novel receptor tyrosine kinase inhibitor for the treatment of gastric cancer. Cancer Lett. 2016 Mar 28;372(2):187-91. [Content Brief]
[3]. Scott LJ. Apatinib: A Review in Advanced Gastric Cancer and Other Advanced Cancers. Drugs. 2018 May;78(7):747-758. doi: 10.1007/s40265-018-0903-9. [Content Brief]
[4]. Tian S, et al. YN968D1 is a novel and selective inhibitor of vascular endothelial growth factor receptor-2 tyrosine kinase with potent activity in vitro and in vivo. Cancer Sci. 2011 Jul;102(7):1374-80. [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 | 2.4660 mL | 12.3298 mL | 24.6597 mL | 61.6492 mL |
| 5 mM | 0.4932 mL | 2.4660 mL | 4.9319 mL | 12.3298 mL | |
| 10 mM | 0.2466 mL | 1.2330 mL | 2.4660 mL | 6.1649 mL | |
| 15 mM | 0.1644 mL | 0.8220 mL | 1.6440 mL | 4.1099 mL | |
| 20 mM | 0.1233 mL | 0.6165 mL | 1.2330 mL | 3.0825 mL | |
| 25 mM | 0.0986 mL | 0.4932 mL | 0.9864 mL | 2.4660 mL | |
| 30 mM | 0.0822 mL | 0.4110 mL | 0.8220 mL | 2.0550 mL | |
| 40 mM | 0.0616 mL | 0.3082 mL | 0.6165 mL | 1.5412 mL | |
| 50 mM | 0.0493 mL | 0.2466 mL | 0.4932 mL | 1.2330 mL | |
| 60 mM | 0.0411 mL | 0.2055 mL | 0.4110 mL | 1.0275 mL |
Apatinib-d8 free base Related Classifications
HY-13342AS Related Classifications
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