761439-42-3 Usage
Biological Activity
tae684 (nvp-tae684) is a selective inhibitor of alk with ic50 value of 3 nm [1].anaplastic lymphoma kinase (alk) is an enzyme and plays an important role in the development of the brain and exerts its effects on specific neurons in the nervous system. it has been reported that alk involves in the pathogenesis of various cancers and serves as an important therapeutic target [1, 2].tae684 (nvp-tae684) is a potent alk inhibitor and has a different selectivity with the reported alk inhibitor crizotinib. when tested with alcl cell lines—karpas-299 and su-dhl-1 expressing npm-alk, tae684 (nvp-tae684) inhibited cell proliferation and cell apoptosis in dose-dependent manner [1]. in lung cancer cell lines harboring wild-type, h694r or e1384k mutant alks, tae684 showed effective inhibition on cell proliferation and phospho-y1604 alk expression of h694r or e1384k mutant alk, but also to a degree higher than that of wild-type alk [2].in scidbeige mice model with luciferized karpas-299 cells subcutaneous xenograft, in which the invasion could be detected by a strong bioluminescence signal, oral administration of tae684 (nvp-tae684) caused significant reduction of lymphoma develop and 100- to 1000-fold reduction in luminecsene signal at the dose of 3 and 10 mg/kg. and, the group received tae684 (nvp-tae684) at the dose of 10 mg/kg appeared healthy and showed no signs of compound- or disease-related toxicity [1].it is also reported that tae684 is a potent inhibitor of leucine-rich repeat kinase 2 (lrrk2) with ic50 value of 7.8 nm [3].
references
[1]. galkin, a.v., et al., identification of nvp-tae684, a potent, selective, and efficacious inhibitor of npm-alk. proc natl acad sci u s a, 2007. 104(1): p. 270-5.[2]. wang, y.w., et al., identification of oncogenic point mutations and hyperphosphorylation of anaplastic lymphoma kinase in lung cancer. neoplasia, 2011. 13(8): p. 704-15.[3]. zhang, j., et al., characterization of tae684 as a potent lrrk2 kinase inhibitor. bioorg med chem lett, 2012. 22(5): p. 1864-9.
Check Digit Verification of cas no
The CAS Registry Mumber 761439-42-3 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 7,6,1,4,3 and 9 respectively; the second part has 2 digits, 4 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 761439-42:
(8*7)+(7*6)+(6*1)+(5*4)+(4*3)+(3*9)+(2*4)+(1*2)=173
173 % 10 = 3
So 761439-42-3 is a valid CAS Registry Number.
InChI:InChI=1/C30H40ClN7O3S/c1-21(2)42(39,40)28-8-6-5-7-26(28)33-29-24(31)20-32-30(35-29)34-25-10-9-23(19-27(25)41-4)37-13-11-22(12-14-37)38-17-15-36(3)16-18-38/h5-10,19-22H,11-18H2,1-4H3,(H2,32,33,34,35)
761439-42-3Relevant academic research and scientific papers
2, 4- DI (PHENYLAMINO) PYRIMIDINES USEFUL IN THE TREATMENT OF NEOPLASTIC DISEASES, INFLAMMATORY AND IMMUNE SYSTEM DISORDERS
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Page 96; 98, (2010/02/08)
Novel pyrimidine derivatives of formula (I), to processes for their production, their use as pharmaceuticals in the treatment of neoplastic diseases, inflammatory and immune system disorders and to pharmaceutical compositions comprising them.
