| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
|
| ln Vitro |
Cells overexpressing ABCG2 benefit from vorolanib (CM082; 1-100 μM) as it potentiates substrate chemistry for fat, however cells overexpressing ABCB1 are unaffected. ABCG2 is unaffected by vorolanib (1.25, 2.5, 5.0, and 20 μM). Vorolanib (0.001–10 μM) suppresses the proliferation of HUVECs induced by VEGF (IC50=0.031 μM) and FBS (IC50= 29.9 μM) [2]. Expression of vorolanib (0.01) at the mRNA or protein level [1]. In vascular endothelial cells, VEGF-induced (40 ng/mL) phosphorylation of VEGFR2 and its downstream signaling pathways ERK1/2, AKT, and STAT3 is concentration-regulatedly inhibited by vorolanib (0.1, 1 μM). has a concentration-dependent effect on the inhibition of FBS-stimulated HUVEC tube formation and cell migration [2].
|
|---|---|
| ln Vivo |
The combination of Vorolanib (CM082; 20 mg/kg; gav; every 2 days; 1 hour before SKF 104864A; for 23 days) and ZD1839 (10 mg/kg; once daily; for 21 days) has been shown to enhance the resistance of SKF 104864A (2 mg/kg; i.p.) to xenografts of ABCG2-overexpressing cells. The results were observed in H3255 tumor xenografts (five-week-old female BALB) [ 1]. It possesses anti-tumor action in naked mice [2].
|
| References |
|
| Additional Infomation |
Vorolanib is under investigation in clinical trial NCT03904719 (CM082 and JS001 in Patients With Advanced Small-cell Lung Cancer (SCLC)).
Vorolanib is an orally available small molecule dual inhibitor targeting human vascular endothelial growth factor receptors (VEGFRs) and platelet-derived growth factor receptors (PDGFRs) with antiangiogenic and antineoplastic activities. Vorolanib inhibits all isoforms of VEGFR and PDGFR, which may result in the inhibition of tumor angiogenesis and tumor cell proliferation, and the induction of tumor cell death. Both VEGFRs and PDGFRs are receptor tyrosine kinases that may be upregulated in various tumor cell types. Vorolanib has been shown to reduce tissue toxicity by 95 percent compared with first-generation kinase inhibitors. |
| Molecular Formula |
C23H26FN5O3
|
|---|---|
| Molecular Weight |
439.4826
|
| Exact Mass |
439.201
|
| CAS # |
1013920-15-4
|
| PubChem CID |
59215954
|
| Appearance |
Light yellow to yellow solid powder
|
| LogP |
1.6
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
32
|
| Complexity |
803
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
FC1C([H])=C([H])C2=C(C=1[H])/C(/C(N2[H])=O)=C(\[H])/C1=C(C([H])([H])[H])C(=C(C([H])([H])[H])N1[H])C(N([H])[C@]1([H])C([H])([H])N(C(N(C([H])([H])[H])C([H])([H])[H])=O)C([H])([H])C1([H])[H])=O
|
| InChi Key |
KMIOJWCYOHBUJS-HAKPAVFJSA-N
|
| InChi Code |
InChI=1S/C23H26FN5O3/c1-12-19(10-17-16-9-14(24)5-6-18(16)27-21(17)30)25-13(2)20(12)22(31)26-15-7-8-29(11-15)23(32)28(3)4/h5-6,9-10,15,25H,7-8,11H2,1-4H3,(H,26,31)(H,27,30)/b17-10-/t15-/m0/s1
|
| Chemical Name |
N-[(3S)-1-(dimethylcarbamoyl)pyrrolidin-3-yl]-5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide
|
| 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 : ~27 mg/mL (~61.44 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.25 mg/mL (5.12 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 22.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2754 mL | 11.3771 mL | 22.7542 mL | |
| 5 mM | 0.4551 mL | 2.2754 mL | 4.5508 mL | |
| 10 mM | 0.2275 mL | 1.1377 mL | 2.2754 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
