5-bromo-indirubins

Abstract

Disclosed herein inter alia are compositions and methods for treating cancer using 5-Br-indirubin derivatives.

1 . A compound, or pharmaceutically acceptable salt thereof, having the formula: 
       
         
           
           
               
               
           
         
         wherein 
         L is an unsubstituted alkylene; 
         R 1  is —NR 2 R 3 ; 
         R 2  and R 3  are joined together to forma substituted or unsubstituted heterocycloalkyl or substituted or unsubstituted heteroaryl; 
         R 5  and R 6  are independently hydrogen. 
       
     
     
         2 .- 5 . (canceled) 
     
     
         6 . The compound of  claim 1 , wherein L is unsubstituted C 2  alkylene. 
     
     
         7 .- 17 . (canceled) 
     
     
         18 . The compound of  claim 1 , wherein R 2  and R 3  are joined together to form a substituted or unsubstituted C 5 -C 7  heterocycloalkyl. 
     
     
         19 . The compound of  claim 18 , wherein R 2  and R 3  are joined together to form a substituted C 5 -C 7  heterocycloalkyl. 
     
     
         20 . The compound of  claim 19 , wherein R 2  and R 3  are joined together to form an R 23 -substituted C 5 -C 7  heterocycloalkyl, wherein R 23  is independently a substituted or unsubstituted alkyl or substituted or unsubstituted heteroalkyl. 
     
     
         21 . The compound of  claim 20 , wherein R 23  is independently a substituted or unsubstituted C 1 -C 8  alkyl or substituted or unsubstituted 2 to 8 membered heteroalkyl. 
     
     
         22 . The compound of claim  16 , wherein R 2  and R 3  are joined together to form a substituted or unsubstituted pyrrolidinyl. 
     
     
         23 . The compound of claim  16 , wherein R 2  and R 3  are joined together to form a substituted or unsubstituted piperazinyl. 
     
     
         24 . The compound of  claim 1  comprising a protonated nitrogen cation or a plurality of protonated nitrogen cations. 
     
     
         25 . (canceled) 
     
     
         26 . (canceled) 
     
     
         27 . The compound of  claim 1  having formula: 
       
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         including pharmaceutical salts thereof. 
       
     
     
         28 . A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of  claim 1 . 
     
     
         29 . The compound of  claim 1  for use in treating cancer in a subject in need thereof. 
     
     
         30 . The compound of  claim 29 , wherein said compound is administered in an effective amount to said subject. 
     
     
         31 . The compound of  claim 29 , wherein said compound is in a pharmaceutical composition comprising a pharmaceutically acceptable excipient. 
     
     
         32 . The compound of  claim 29 , wherein said cancer is lung cancer, breast cancer, ovarian cancer, leukemia, lymphoma, melanoma, pancreatic cancer, sarcoma, bladder cancer, bone cancer, brain cancer, cervical cancer, colon cancer, esophageal cancer, gastric cancer, liver cancer, head and neck cancer, kidney cancer, myeloma, thyroid cancer, or prostate cancer. 
     
     
         33 . The compound of  claim 29 , wherein said compound is co-administered with an effective amount of an anti-cancer agent. 
     
     
         34 . A method of modulating a kinase, a JAK, JAK2, TYK2, Src, c-Src, ABL1, ABL1 T315I, an Aurora kinase, Aurora A, GSK-3β, a CDK, a STAT, or STAT3, said method comprising contacting the protein with the compound of  claim 1 . 
     
     
         35 . The method of  claim 34 , wherein the compound is in a pharmaceutical composition comprising a pharmaceutically acceptable excipient. 
     
     
         36 . A method of modulating a Janus kinase, said method comprising contacting said Janus kinase with the compound of  claim 1 . 
     
     
         37 . The method of  claim 36 , wherein the compound is in a pharmaceutical composition comprising a pharmaceutically acceptable excipient.