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Elzovantinib (TPX0022; TPX-0022; CSF1R-IN-2) is a novel and potent multi-kinase inhibitor of SRC, MET and c-FMS (IC50 = 0.12 nM, 0.14 nM and 0.76 nM for SRC, MET and c-FMS respectively) with anticancer activity.
| ln Vitro |
In SNU-5 and MKN-45 cell lines, elzovantinib (TPX-0022) suppresses MET autophosphorylation as well as downstream phosphorylation of STAT3, ERK, and AKT at IC50 values of approximately 1-3 nM[1].
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| ln Vivo |
In mice treated for 21 days, ezovantinib (TPX-0022; po, BID, 13 days) causes an 85% tumor shrinkage and no loss of body weight[1]. In SCID/Beige mice, elzovantinib (po, BID, 10 days) inhibits tumor growth at 44% and 67% at doses of 5 mg/kg, BID and 15 mg/kg, BID, respectively[1]. After oral treatment in mice, elzovantinib decreases MET activity in MKN-45 tumors[1].
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| Animal Protocol |
Animal/Disease Models: Mice bearing LU2503 tumors patient derived xenograft (PDX) NSCLC model[1].
Doses: 15 mg/kg. Route of Administration: PO, BID (twice (two times) daily) for 13 days. Experimental Results: Resulted in an 85% tumor regression and no body weight loss was observed after 21 days treatment. Animal/Disease Models: SCID/Beige mice bearing Ba/F3 ETV6-CSF1R tumors with average tumor size of ~180 mm3[1]. Doses: 5 and 15 mg/ kg. Route of Administration: PO, BID (twice (two times) daily) for 10 days. Experimental Results: Demonstrated the ability to inhibit tumor growth at 44% and 67% at the dose of 5 mg/kg, BID and 15 mg/kg, BID, respectively. |
| References | |
| Additional Infomation |
Elzovantinib is an orally bioavailable, multi-targeted kinase inhibitor with potential antineoplastic activity. Upon oral administration, elzovantinib binds to and inhibits three tyrosine kinases that are often overexpressed in a variety of cancer cell types, including MET (c-Met; hepatocyte growth factor receptor; HGFR) , Src, and colony stimulating factor 1 receptor (CSF1R; CSF-1R; C-FMS; CD115; macrophage colony-stimulating factor receptor; M-CSFR) thereby disrupting their respective signaling pathways. MET, a receptor tyrosine kinase overexpressed or mutated in many tumor cell types, plays an important role in tumor cell proliferation, survival, invasion, and metastasis, and in tumor angiogenesis. Src, a non-receptor tyrosine kinase upregulated in many tumor cell types, plays an important role in tumor cell proliferation, motility, invasiveness and survival. CSF1R is a cell-surface receptor for colony stimulating factor 1 (CSF1); this receptor tyrosine kinase is overexpressed by tumor-associated macrophages (TAMs) in the tumor microenvironment (TME), and plays a major role in both immune suppression and the induction of tumor cell proliferation.
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| Molecular Formula |
C20H20FN7O2
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|---|---|
| Molecular Weight |
409.416906356812
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| Exact Mass |
409.17
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| Elemental Analysis |
C, 58.67; H, 4.92; F, 4.64; N, 23.95; O, 7.82
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| CAS # |
2271119-26-5
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| PubChem CID |
137455315
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| Appearance |
White to off-white solid powder
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| LogP |
2.1
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
30
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| Complexity |
687
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CCN1CC2=C(C=CC(=C2C#N)F)O[C@H](CNC(=O)C3=C4N=C1C=CN4N=C3N)C
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| InChi Key |
UUDPUQDMSHQSKH-NSHDSACASA-N
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| InChi Code |
InChI=1S/C20H20FN7O2/c1-3-27-10-13-12(8-22)14(21)4-5-15(13)30-11(2)9-24-20(29)17-18(23)26-28-7-6-16(27)25-19(17)28/h4-7,11H,3,9-10H2,1-2H3,(H2,23,26)(H,24,29)/t11-/m0/s1
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| Chemical Name |
(S,13E,14E)-12-amino-2-ethyl-45-fluoro-6-methyl-9-oxo-5-oxa-2,8-diaza-1(5,3)-pyrazolo[1,5-a]pyrimidina-4(1,2)-benzenacyclononaphane-46-carbonitrile
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| Synonyms |
TPX0022 CSF1R-IN-2TPX 0022 CSF1R-IN2TPX-0022 Elzovantinib
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~61.06 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.08 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 20.8 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. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.08 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4425 mL | 12.2124 mL | 24.4248 mL | |
| 5 mM | 0.4885 mL | 2.4425 mL | 4.8850 mL | |
| 10 mM | 0.2442 mL | 1.2212 mL | 2.4425 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.
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