Size | Price | Stock | Qty |
---|---|---|---|
5mg |
|
||
10mg |
|
||
25mg |
|
||
50mg |
|
||
100mg |
|
||
250mg |
|
||
500mg |
|
||
Other Sizes |
|
Ningetinib, also known as CT-053, is a potent, orally bioavailable small molecule tyrosine kinase inhibitor (TKI) with IC50s of 6.7, 1.9 and<1.0 nM for c-Met, VEGFR2 and Axl, respectively.
Targets |
Axl (IC50 = 1.0 nM); VEGFR2 (IC50 = 1.9 nM); c-Met (IC50 = 6.7 nM)
|
---|---|
ln Vitro |
Ningetinib is a strong small molecule tyrosine kinase inhibitor (TKI) that is orally bioavailable. Its IC50 values for c-Met, VEGFR2, and Axl are 6.7, 1.9, and less than 1.0 nM, respectively. With IC50 values of 8.6 and 6.3 nM, respectively, neingetinib (CT053PTSA) inhibited HGF- and VEGF-stimulated HUVEC proliferation and microangiogenesis in arterial rings in cell-based functional assays [1].
|
ln Vivo |
Giving nintegetinib (CT053PTSA) as a single intraventricular injection (3 mg/kg) to tumor-bearing U87MG nude mice successfully suppressed the phosphorylation of c-Met and its downstream signaling pathways AKT and ERK1/2 in tumor tissue for 6 hours. A damaging dose of 20 mg/kg/day (21 days of medication use) of nigatinib significantly raised the consumption value (ILS=32%, p=0.003) and lengthened the median survival time (MST) in the orthotopic U87MG human astrocytoblastoma xenograft model[1].
|
References |
[1]. Ning Xi, et al. Abstract 1755: CT053PTSA, a novel c-MET and VEGFR2 inhibitor, potently suppresses angiogenesis and tumor growth. Cancer Res 2014;74(19 Suppl):Abstract nr 1755.
|
Molecular Formula |
C₃₁H₂₉FN₄O₅
|
---|---|
Molecular Weight |
556.58
|
Exact Mass |
556.21
|
Elemental Analysis |
C, 62.63 H, 5.12 F, 2.61 N, 7.69 O, 17.56,S, 4.40
|
CAS # |
1394820-69-9
|
Related CAS # |
Ningetinib Tosylate;1394820-77-9
|
Appearance |
Solid powder
|
SMILES |
CC1=C(C(=O)N(N1C)C2=CC=CC=C2)C(=O)NC3=CC(=C(C=C3)OC4=C5C=CC(=CC5=NC=C4)OCC(C)(C)O)F
|
InChi Key |
VQYYQSZNRVQLIS-UHFFFAOYSA-N
|
InChi Code |
InChI=1S/C31H29FN4O5/c1-19-28(30(38)36(35(19)4)21-8-6-5-7-9-21)29(37)34-20-10-13-27(24(32)16-20)41-26-14-15-33-25-17-22(11-12-23(25)26)40-18-31(2,3)39/h5-17,39H,18H2,1-4H3,(H,34,37)
|
Chemical Name |
N-[3-fluoro-4-[7-(2-hydroxy-2-methylpropoxy)quinolin-4-yl]oxyphenyl]-1,5-dimethyl-3-oxo-2-phenylpyrazole-4-carboxamide
|
Synonyms |
Ningetinib Tosylate; CT-053 Tosylate; CT-053; DE-120; CT053; DE120; CT 053; DE 120
|
HS Tariff Code |
2934.99.9001
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
DMSO: 16.7~20 mg/mL (30~35.9 mM)
|
---|---|
Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.7967 mL | 8.9834 mL | 17.9669 mL | |
5 mM | 0.3593 mL | 1.7967 mL | 3.5934 mL | |
10 mM | 0.1797 mL | 0.8983 mL | 1.7967 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT04992858 | Not yet recruiting | Drug: CT053PTSA | Advanced NSCLC | Sunshine Lake Pharma Co., Ltd. | November 27, 2022 | Phase 2 |
NCT03758287 | Active Recruiting |
Drug: CT053PTSA Drug: Gefitinib |
Non-small Cell Lung Cancer | Sunshine Lake Pharma Co., Ltd. | November 2016 | Phase 1 Phase 2 |
NCT04577703 | Completed | Drug: CT053PTSA | Advanced Solid Tumors | Sunshine Lake Pharma Co., Ltd. | February 8, 2014 | Phase 1 |
NCT03125876 | Terminated | Drug: CT053PTSA | Acute Myeloid Leukemia (AML) |
Sunshine Lake Pharma Co., Ltd. | November 13, 2017 | Phase 1 |