1001350-96-4 Usage
Description
BMS-754807 is a pyrrolotriazine that functions as a potent and reversible dual inhibitor of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (InsR) tyrosine kinases. It is an orally bioavailable compound with minimal effects on other tyrosine and serine/threonine kinases. BMS-754807 acts as an ATP-competitive antagonist by restricting the catalytic domain of the IGF-1R, thereby inhibiting cell proliferation and inducing apoptosis in various cancer cells. It has been found to be effective in inhibiting the growth of tumor xenografts in mice, with its efficacy often enhanced by combination therapy with other chemotherapeutic agents.
Uses
Used in Pharmaceutical Industry:
BMS-754807 is used as an IGF-1R inhibitor for its ability to inhibit cell proliferation and induce apoptosis in a variety of cancer cells. It has demonstrated effectiveness in embryo drug treatment and has an IC50 of 13 nM.
Used in Cancer Treatment:
BMS-754807 is used as a dual inhibitor of IGF-1R and InsR tyrosine kinases for its potential to inhibit the growth of tumor xenografts in mice. Its effectiveness is often enhanced when used in combination with other chemotherapeutic drugs, and predictive biomarkers, such as elevated IGF-1R expression, have been identified for its therapeutic success.
Used in Drug Development:
BMS-754807 is utilized in the development of novel drug delivery systems to improve its delivery, bioavailability, and therapeutic outcomes in cancer treatment. Various organic and metallic nanoparticles have been explored as carriers for BMS-754807, aiming to enhance its overall efficacy against cancer cells.
Biochem/physiol Actions
BMS-754807 is an orally available and potent dual insulin-like growth factor factor-1 receptor (IGF-1R)/ insulin receptor (InsR) tyrosine kinase inhibitor that synergistically enhances antiproliferative effects of 4-hydroxytamoxifen, letrozole, and fulvestrant in MCF-7/AC-1 cells.
references
[1] q.s. chu，s.w. kim，p.m. ellis，l. mileshkin，r.h. de boer，j.s. park，t. pellas，f. huang，f. graf finckenstein，a. dhar. bms-754807, an oral dual igf-1r/insulin receptor (ir) inhibitor: initial results from a phase 1 dose- and schedule-?nding study in combination with carboplatin/paclitaxel in subjects with solid tumors. european journal of cancer supplements. november 2010, 8(7): 131.[2] vattoly j. majo, victoria arango, norman r. simpson, jaya prabhakaran, suham a. kassir, mark d. underwood, mihran bakalian, peter canoll, j. john mann, j.s. dileep kumar. synthesis and in vitro evaluation of [18f]bms-754807: a potential pet ligand for igf-1r. bioorganic & medicinal chemistry letters. july 2013, 23(14): 4191-4194.[3] joan m. carboni, mark wittman, zheng yang, et al.. bms-754807, a small molecule inhibitor of insulin-like growth factor-1r/ir. mol cancer ther. 2009;8:3341-3349.
Check Digit Verification of cas no
The CAS Registry Mumber 1001350-96-4 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,0,0,1,3,5 and 0 respectively; the second part has 2 digits, 9 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 1001350-96:
(9*1)+(8*0)+(7*0)+(6*1)+(5*3)+(4*5)+(3*0)+(2*9)+(1*6)=74
74 % 10 = 4
So 1001350-96-4 is a valid CAS Registry Number.
