942487-16-3 Usage
Description
The Aurora kinases are a family of serine/threonine kinases that are key regulators of mitosis and cytokinesis. PF-03814735 is a reversible inhibitor of both Aurora A and B kinases with IC50 values of 0.8 and 5 nM, respectively, in in vitro activity assays. PF-03814735 also inhibits the kinases FLT1, FAK, TrkA, Met, and FGFR1 with IC50 values of 10, 22, 30, 100, and 100 nM, respectively. PF-03814735 inhibits cell proliferation of HCT116, HL-60, A549, and H125 tumor cell lines with IC50 values ranging from 42-150 nM and shows in vivo efficacy in an HCT116 tumor xenograft mouse model. PF-03814735 has been shown to be particularly sensitive towards inhibiting the growth of small cell lung cancer cell lines and other tumors driven by the Myc family genes.
Chemical Properties
Off-White Solid
Uses
Different sources of media describe the Uses of 942487-16-3 differently. You can refer to the following data:
1. PF 03814735 is an orally bioavailable small molecule aurora kinase inhibitor that plays a key role in the regulation of mitosis. PF 03814735 is a anticancer agent used for cancer therapy.
2. The Aurora kinases are a family of serine/threonine kinases that are key regulators of mitosis and cytokinesis. PF-03814735 is a reversible inhibitor of both Aurora A and B kinases with IC50 values of 0.8 and 5 nM, respectively, in in vitro activity assays. PF-03814735 also inhibits the kinases FLT1, FAK, TrkA, Met, and FGFR1 with IC50 values of 10, 22, 30, 100, and 100 nM, respectively. PF-03814735 inhibits cell proliferation of HCT-116, HL-60, A549, and H125 tumor cell lines with IC50 values ranging from 42-150 nM and shows in vivo efficacy in an HCT-116 tumor xenograft mouse model. PF-03814735 has been shown to be particularly sensitive towards inhibiting the growth of small cell lung cancer cell lines and other tumors driven by the Myc family genes.[Cayman Chemical]
references
[1] jani jp, arcari j, bernardo v, bhattacharya sk, briere d, cohen bd, coleman k, christensen jg, emerson eo, jakowski a, hook k, los g, moyer jd, pruimboom-brees i, pustilnik l, rossi am, steyn sj, su c, tsaparikos k, wishka d, yoon k, jakubczak jl. pf-03814735, an orally bioavailable small molecule aurora kinase inhibitor for cancer therapy. mol cancer ther. 2010 apr;9(4):883-94.
Check Digit Verification of cas no
The CAS Registry Mumber 942487-16-3 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 9,4,2,4,8 and 7 respectively; the second part has 2 digits, 1 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 942487-16:
(8*9)+(7*4)+(6*2)+(5*4)+(4*8)+(3*7)+(2*1)+(1*6)=193
193 % 10 = 3
So 942487-16-3 is a valid CAS Registry Number.
942487-16-3Relevant articles and documents
PYRIMIDINE DERIVATIVES FOR THE TREATMENT OF ABNORMAL CELL GROWTH
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Page/Page column 102, (2010/11/27)
The present invention relates to a compound of the formula (I), or a pharmaceutically acceptable salt thereof, wherein Ar is a group of formula (III), and R1, R2, R13, A, K, M, L1, L2, X, Y1, Y2, Q, salt thereof, wherein R1, R2, R13, A, K, L1, L2, W, X, Z1, Z2, Y1, Y2, Z1, Z2, M, Q, W, X, m, p and q are as defined herein. Such novel pyrimidine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.