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. 2016 Aug 1;10:2443–2459. doi: 10.2147/DDDT.S89114

Table 5.

c-Kit inhibitors classification based on their targets, chemical and structure formulae, and diseases they are tested on

Name Targets IC50a (nM) Structure Formula Molecular weight (g/mol) Chemical name FDA-approved inhibitor Clinical trial information testing on
Amuvatinib (MP-470) c-Kit, PDGFRα, Flt3 10, 40, 81 graphic file with name dddt-10-2443Fig12.jpg C23H21N5O3S 447.51 Not mentioned Approved by the FDA for CML, GISTs and a number of other malignancies Lymphoma, unspecified adult solid tumor, solid tumors, malignant disease, small-cell lung carcinoma
Axitinib VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit 0.1, 0.2, 0.1–0.3, 1.6, 1.7 graphic file with name dddt-10-2443Fig13.jpg C22H18N4OS 386.47 Approved by the FDA Advanced renal cell carcinoma, renal cell carcinoma, nonclear cell, temsirolimus-resistant renal cell carcinoma, pheochromocytoma, paraganglioma, advanced solid tumors
Cabozantinib (XL184, BMS-907351) VEGFR2, c-Met, Ret, Kit, Flt-1/3/4, Tie2, AXL 0.035, 1.3, 4, 4.6, 12/11.3/6, 14.3, 7 graphic file with name dddt-10-2443Fig14.jpg C28H24FN3O5 501.51 Approved by the FDA for renal cell carcinoma Medullary thyroid cancer, prostate cancer, castration-resistant prostate cancer, prostatic neoplasms, colorectal cancer, uterine sarcoma, and prostate cancer
Dasatinib Abl, Src, c-Kit 1, 0.8, 79 graphic file with name dddt-10-2443Fig15.jpg C22H26ClN7O2S 488.01 Approved by the FDA for Ph+ CML AML, breast cancer, recurrent childhood brain tumor, lung cancer/NSCLC, chronic myeloid leukemia
Dovitinib (TKI-258, CHIR-258) FLT3, c-Kit, FGFR1/3, VEGFR1-4, InsR, EGFR, c-Met, EphA2, Tie2, IGF-1R, and HER2 1/2, 8–13 graphic file with name dddt-10-2443Fig16.jpg C21H21FN6O 392.43 Propanoic acid, 2-hydroxy-, compound with 4-amino-5-fluoro-3-[6-(4-methyl-1-piperazinyl)- 1H-benzimidazol-2-yl]-2(1H)-quinolinone
a

The IC50 is a measure of the effectiveness of a substance in inhibiting a specific biological or biochemical function.

Abbreviations: IC50, half-maximal inhibitory concentration; FDA, Food and Drug Administration; CML, chronic myelogenous leukemia; GIST, gastrointestinal stromal tumor; AML, acute myeloid leukemia; NSCLC, non-small-cell lung cancer.