1. Protein Tyrosine Kinase/RTK
    Autophagy
  2. VEGFR
    Autophagy

Apatinib (Synonyms: YN968D1)

Cat. No.: HY-13342 Purity: 99.76%
Data Sheet SDS Handling Instructions

Apatinib is a selective VEGFR2 inhibitor with IC50 of 1 nM. Apatinib also potently suppresses the activities of Ret, c-Kit and c-Src with IC50s of 13, 429 and 530 nM, respectively. Apatinib has no significant effects on EGFR, Her-2 or FGFR1 in concentrations up to 10 μM.

For research use only. We do not sell to patients.
Apatinib Chemical Structure

Apatinib Chemical Structure

CAS No. : 1218779-75-9

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10 mM * 1 mL in DMSO $121 In-stock
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10 mg $150 In-stock
50 mg $350 In-stock
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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Apatinib is a selective VEGFR2 inhibitor with IC50 of 1 nM. Apatinib also potently suppresses the activities of Ret, c-Kit and c-Src with IC50s of 13, 429 and 530 nM, respectively. Apatinib has no significant effects on EGFR, Her-2 or FGFR1 in concentrations up to 10 μM.

IC50 & Target

IC50: 1 nM (VEGFR2), 13 nM (Ret), 429 nM (c-Kit), 530 nM (c-Src)[1]

In Vitro

Apatinib (YN968D1) slightly inhibits proliferation of HUVEC stimulated by 20% FBS (IC50=23.4 μM), whereas Apatinib significantly inhibits proliferation stimulated by 20 ng/mL VEGF (IC50=0.17 μM). The IC50 values of Sunitinib are lower under the same conditions (7.4 μM and 0.034 μM, respectively). 1 μM Apatinib significantly inhibits the migration of HUVEC induced by FBS, but does not affect proliferation of HUVEC, indicating that the inhibitory effect of Apatinib on FBS-induced migration is not due to the suppression of proliferation. At a concentration of 1 μM, Sunitinib also inhibits the migration of HUVEC[1].

In Vivo

The antitumor potential of Apatinib (YN968D1) is evaluated in six human tumor xenografts in immunodeficient mice. Once-daily oral administration of Apatinib produces a dose-dependent inhibition of tumor growth in all tumor models examined. Statistically significant growth inhibition is obtained with 50 mg/kg per day Apatinib in three of five tumor xenografts tested. Each tumor xenograft model is significantly growth inhibited by Apatinib at the dose of 100 kg/day. Similar tumor growth inhibition is observed (T/C%, 8% to 18%) in mice following treatment with Apatinib at the dose of 200 kg/day. Full growth inhibition profiles are shown for three of the xenografts. Compared with the control animals, no effect of Apatinib treatment on bodyweight is observed at any dose level, which suggested that Apatinib is well tolerated[1].

Clinical Trial
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References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.0260 mL 10.1301 mL 20.2601 mL
5 mM 0.4052 mL 2.0260 mL 4.0520 mL
10 mM 0.2026 mL 1.0130 mL 2.0260 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[1]

Apatinib (YN986D1) is dissolved in DMSO and stored, and then diluted with appropriate medium before use[1].

The following human tumor cell lines are used: Ls174t, HCT 116, SGC-7901, HT-29, A549, NCI-H460, Mo7e, A431, BT474 and NIH-3T3. The cells are cultured in RPMI-1640 or DMEM supplemented with 10% FBS at 37°C with 5% carbon dioxide. Primary HUVEC are isolated from segments of normal-term cords by digestion with type I collagenase, and are pooled and cultured in Medium 199 (M199) supplemented with 20% FBS and endothelial cell growth factor. Cells in the exponential growth phase are used in the experiments. The HUVEC are seeded into 96-well plates. After 24 h of incubation, cells are exposed to the test agents (vehicle as control) together with 20 ng/mL VEGF or 20% FBS for another 72 h. After fixation with 10% trichloroacetic acid, the cells are stained with 0.4% sulforhodamine B for 30 min at 37°C and then washed with 1% acetic acid. Tris is added to dissolve the complex, and the optical density is measured at 520 nm[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Apatinib (YN986D1) is diluted in 0.5% (w/v) carboxymethyl cellulose and 5% (w/v) glucose solution (Mice)[1].

Mice[1]
The effects of Apatinib (YN968D1) on tumor growth are tested against various human tumors grown subcutaneously in BALB/cA nude mice. Tumor growth is initiated by subcutaneous inoculation of cells into mice. Tumors are allowed to establish and grow to 100-300 mm3, at which time the mice are randomized into experimental groups. Apatinib is administered once daily by oral gavage for the indicated periods. In combination treatment experiments, mice are administered Apatinib alone by oral gavage; 5-FU, oxaliplatin, docetaxel and doxorubicin alone by intravenous injection; or Apatinib in combination with each cytotoxic drug at the indicated dose and schedule. Tumor volume and bodyweight are monitored every other day or every 3 days, with the means indicated for groups of six (treated) or 12 (vehicle control) animals. Tumor volumes are determined by measuring the largest diameter (a) and its perpendicular (b) according to the formula (a×b2)/2. The evaluation index for inhibition is the relative tumor growth ratio according to the equation: T/C (%)=mean increase of tumor volumes of treated groups⁄mean increase of tumor volumes of control groups×100%. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

493.58

Formula

C₂₅H₂₇N₅O₄S

CAS No.

1218779-75-9

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 32 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.76%

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Apatinib
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