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AXL-IN-13 is a potent and orally active AXL inhibitor with an IC50 of 1.6 nM and a Kd of 0.26 nM. It exhibits anticancer activity, reverses TGF-β1-induced epithelial-mesenchymal transition (EMT), and inhibits cancer cell migration and invasion.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $79 | In Stock | |
5 mg | $190 | In Stock | |
10 mg | $280 | In Stock | |
25 mg | $480 | In Stock | |
50 mg | $687 | In Stock | |
100 mg | $998 | In Stock | |
500 mg | $1,990 | In Stock |
Description | AXL-IN-13 is a potent and orally active AXL inhibitor with an IC50 of 1.6 nM and a Kd of 0.26 nM. It exhibits anticancer activity, reverses TGF-β1-induced epithelial-mesenchymal transition (EMT), and inhibits cancer cell migration and invasion. |
Targets&IC50 | Axl:1.6 nM, PDGFRβ:2.3 nM (Kd) |
In vitro | AXL-IN-13 (Compound 6li) inhibits Ba/F3-TEL-AXL cell proliferation with an IC50 of 4.7 nM (as determined by ELISA).[1] AXL-IN-13 (0-500 nM; 6 hours) inhibits AXL phosphorylation in MDA-MB-231 and 4T1 cells.[1] AXL-IN-13 also shows binding affinity for CSF1R, FLT1/3/4, KLT, PDGFRB, TIE2.[1] AXL-IN-13 (0-3 μM; 3 days) blocks TGF-β1 (10 ng/mL)-induced EMT in MDA-MB-231 cells.[1] AXL-IN-13 (0-3 μM; 24 hours) inhibits TGF-β1 (10 ng/mL)-induced migration and invasion of MDA-MB-231 cells.[1] |
In vivo | AXL-IN-13 (Compound 6li) (50 or 100 mg/kg; p.o.; 14 days; Xenograft model derived from highly metastatic 4T1 cells) inhibits 4T1 tumor growth and metastasis.[1] AXL-IN-13 (25 mg/kg; oral; Xenograft model derived from highly metastatic 4T1 cells) shows a good PK curve, with an AUC of 8410.21 ng/mL/h, a T1/2 value of 4.22 h, and an oral bioavailability (F) of 14.4%.[1] |
Molecular Weight | 632.72 |
Formula | C34H41FN6O5 |
Cas No. | 2376928-82-2 |
Smiles | O(C=1C2=C(C=C(OCCCN3CCOCC3)C(OC)=C2)N=CC1)C4=C(F)C=C(NC=5C(C(NC6CCCCC6)=O)=CN(C)N5)C=C4 |
Storage | Shipping with blue ice. | ||||||||||||||||||||
Solubility Information | DMSO: 6.33 mg/mL (10 mM), Sonication is recommended. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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