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Cabozantinib hydrochloride

Catalog No. T5164   CAS 1817759-42-4
Synonyms: XL184, Cabozantinib hydrochloride (849217-68-1(free base)), BMS-907351

Cabozantinib hydrochloride (XL184) is a potent pan-tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt4 (IC50s: 0.035, 1.3, 4.6, 7 and 6 nM).

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Cabozantinib hydrochloride Chemical Structure
Cabozantinib hydrochloride, CAS 1817759-42-4
Pack Size Availability Price/USD Quantity
1 mg In stock $ 37.00
2 mg In stock $ 50.00
5 mg In stock $ 63.00
10 mg In stock $ 98.00
25 mg In stock $ 172.00
50 mg In stock $ 260.00
100 mg In stock $ 367.00
200 mg In stock $ 598.00
500 mg In stock $ 956.00
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Purity: 97.09%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Cabozantinib hydrochloride (XL184) is a potent pan-tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt4 (IC50s: 0.035, 1.3, 4.6, 7 and 6 nM).
Targets&IC50 RORγ:111 nM (Ki), RORα:172 nM (Ki)
In vitro SR1001 binds specifically to the ligand-binding domains of RORα and RORγt, inducing a conformational change within the ligand-binding domain, resulting in suppression of the receptors' transcriptional activity. SR1001 inhibited the development of murine T(H)17 cells. Furthermore, SR1001 inhibited the expression of cytokines when added to differentiated murine or human T(H)17 cells [1]. Treatment with the RORγT inhibitor SR1001 to abrogate Th17 cell function reduced Th17-dependent learned helplessness [2].
In vivo After myelin oligodendrocyte glycoprotein (MOG35–55) immunization at day 0, experimental autoimmune encephalomyelitis (EAE) mice were treated with SR1001 (25 mg/kg, b.i.d. i.p.) for the duration of the study. Further analysis of spinal cords from mice harvested at day 18 post-immunization revealed that SR1001 repressed Il17a mRNA expression by ~60%, as well as reduced Il21, and Il22 mRNA expression [1]. When these mice were injected with SR1001, the circadian rhythm of CS expression was eliminated [3].
Cell Research CD4+ T cells were isolated as described previously and in the Supplementary Materials. CD4+ T cells cultured with splenic feeder cells were activated with 2.5 μg/mL of anti-CD3 (clone 145–11), and differentiated to Th17 cells by addition of IL-6 (20 ng/mL; Peprotech), TGFβ (5 ng/mL), anti-IL-4 (10 μg/mL; clone 11B11, UAB core facility) and anti-IFNγ (10 μg/mL; clone XMG1.2, UAB core facility). After 5 days of differentiation toward Th17 cells, cells were recovered after histopaque gradient purification and resuspended in PBS. An aliquot of cells was used to evaluate the percent of Th17 cells (~40%) and ~10–20×106 undifferentiated CD4+ T or Th17 cells were injected in 500 μL PBS by tail vein 48 h prior to behavioral testing. Where indicated, mice were injected intraperitoneally with 100 μg anti-IL-17A, or 125 μg SR1001 daily beginning 1 day before Th17 cell transfer, and this was continued throughout the experiment. As controls, mice were injected i.v. with ~10–20×106 CD4+ T cells to evaluate the effect of non-differentiated cells, or with 500 μL PBS to mimic the stress of tail vein i.v. injection 48 h prior to behavioral testing. Intracellular cytokine staining was carried out as described previously and in the Supplementary Information [2].
Animal Research For circadian gene expression experiments male C57BL6 mice (8–10 weeks of age) were either maintained on a L:D (12h∶12h) cycle or on constant darkness (1 day). At the circadian time (CT) 0 animals were administered a single dose of 25 mg/kg SR1001 (i.p.) and groups of animals (n?=?6) were sacrificed at CT0, CT6, CT12, and CT18. Gene expression was determined by real-time qPCR. Gene expression was normalized to Cyclophin b in all experiments [3].
Synonyms XL184, Cabozantinib hydrochloride (849217-68-1(free base)), BMS-907351
Molecular Weight 537.96
Formula C28H25ClFN3O5
CAS No. 1817759-42-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 80 mg/mL

TargetMolReferences and Literature

1. Yakes FM, et al. Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth. Mol Cancer Ther, 2011, 10(12), 2298-2308. 2. Torres KE, et al. Activated MET is a molecular prognosticator and potential therapeutic target for malignant peripheral nerve sheath tumors.Clin Cancer Res. 2011 Jun 15;17(12):3943-55. 3. You WK, et al. VEGF and c-Met blockade amplify angiogenesis inhibition in pancreatic islet cancer. Cancer Res, 2011, 71(14), 4758-4768.

Related compound libraries

This product is contained In the following compound libraries:
Tyrosine Kinase Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Anti-Breast Cancer Compound Library Bioactive Compound Library Anti-Metabolism Disease Compound Library Drug Repurposing Compound Library Inhibitor Library

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Keywords

Cabozantinib hydrochloride 1817759-42-4 Angiogenesis Metabolism Tyrosine Kinase/Adaptors FLT c-Met/HGFR VEGFR c-Kit TAM Receptor ROR inhibit CD135 Mer Fms like tyrosine kinase 3 Inhibitor XL184 SCFR BMS 907351 Axl XL 184 Cluster of differentiation antigen 135 XL-184 Vascular endothelial growth factor receptor Cabozantinib hydrochloride (849217-68-1(free base)) angiogenesis CD117 BMS-907351 BMS907351 FLT3 HT1080 Cabozantinib Hydrochloride A431 antiangiogenic Apoptosis Tyro3 Cabozantinib B16F10 cells inhibitor

 

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