1. Protein Tyrosine Kinase/RTK Autophagy
  2. Src VEGFR Autophagy c-Kit RET
  3. Apatinib-d8 free base

Apatinib-d8 free base  (Synonyms: YN968D1-d8 free base)

Cat. No.: HY-13342AS Purity: 92.56%
SDS COA Handling Instructions

Apatinib-d8 (free base) is the deuterium labeled Apatinib free base[1]. 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[2][3][4].

For research use only. We do not sell to patients.

Apatinib-d<sub>8</sub> free base Chemical Structure

Apatinib-d8 free base Chemical Structure

CAS No. : 2468771-43-7

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1 mg USD 120 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Apatinib-d8 (free base) is the deuterium labeled Apatinib free base[1]. 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[2][3][4].

In Vitro

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.

Molecular Weight

405.52

Formula

C24H15D8N5O

CAS No.
Unlabeled CAS

811803-05-1

Appearance

Solid

Color

Off-white to light yellow

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

Shipping

Room temperature in continental US; may vary elsewhere.

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
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4660 mL 12.3298 mL 24.6597 mL
5 mM 0.4932 mL 2.4660 mL 4.9319 mL
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Purity & Documentation
References

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
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Apatinib-d8 free base
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