1123837-84-2 Usage
Description
Sitravatinib, also known as MGCD516, is a multikinase inhibitor that targets various receptor tyrosine kinases, including MET, RET, AXL, NTRK1, and NTRK3. It has been evaluated in phase 1/1b clinical trials for the treatment of advanced cancers and has demonstrated the ability to reduce the proliferation of several cancer cell lines and decrease tumor growth in mouse xenograft models.
Uses
Used in Oncology:
Sitravatinib is used as an anticancer agent for the treatment of advanced cancers. It inhibits the activity of multiple receptor tyrosine kinases, which are often dysregulated in cancer cells, leading to reduced cell proliferation and tumor growth inhibition.
Used in Drug Development:
Sitravatinib serves as an intermediate in the preparation of substituted thienopyridines, which are inhibitors of protein tyrosine kinase activity. This makes it a valuable compound in the development of new therapeutic agents targeting kinase-mediated signaling pathways in various diseases, including cancer.
Used in Preclinical Research:
In preclinical studies, Sitravatinib has been shown to reduce the proliferation of various cancer cell lines, such as A-673, LPS141, MPNST, DDLS, and Saos-2, and decrease the phosphorylation of key signaling proteins like IGF1-R, PDGFRβ, and Akt. This makes it a useful tool for investigating the role of these kinases in cancer progression and for testing potential combination therapies in preclinical models.
References
1) Parag?et al.?(2016)?Significant blockade of multiple receptor kinases by MGCD516 (Sitravatinib), a novel small molecule inhibitor, shows potent anti-tumor activity in preclinical models of sarcoma; Oncotarget?7?4093
2) Leal?et al.?(2017)?Evidence of clinical activity of sitravatinib in combination with nivolumab in NSCLC patients progressing on prior checkpoint inhibitors; J. Thorac. Oncol.?12?S1803
3) Du?et al.?(2018);?Sitravatinib potentiates immune checkpoint blockade in refractory cancer models; JCI Insight?3?124184
Check Digit Verification of cas no
The CAS Registry Mumber 1123837-84-2 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,1,2,3,8,3 and 7 respectively; the second part has 2 digits, 8 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 1123837-84:
(9*1)+(8*1)+(7*2)+(6*3)+(5*8)+(4*3)+(3*7)+(2*8)+(1*4)=142
142 % 10 = 2
So 1123837-84-2 is a valid CAS Registry Number.
1123837-84-2Relevant articles and documents
TREATMENT OF CANCER WITH ANTI-OX40 ANTIBODIES AND MULTI-KINASE INHIBITORS
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, (2021/05/29)
The present disclosure provides methods of treating cancer with non-competitive, agonist anti-OX40 antibodies and antigen-binding fragments thereof that bind to human OX40 (ACT35, CD134, or TNFRSF4), in combination with a multi-kinase inhibitor.
INHIBITORS OF PROTEIN TYROSINE KINASE ACTIVITY
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Page/Page column 114-115, (2009/04/25)
The invention relates to compounds of Formula (I) and their use for inhibiting protein tyrosine kinase activity In Formula (I), the group M is thieno[3,2,b]pyridinyl as shown, and the group D is a ring or ring system, and the groups Z, Ar, and G are as defined herein The invention relates particularly to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signalling, for example, the inhibition of VEGF receptor signalling and HGF receptor signalling The invention also provides compositions and methods for treating cell proliferative diseases and conditions, such as cancer, and for treating ophthalmic diseases, including age-related macular degeneration (AMD) and diabetic retinopathy (DR)
