Anlotinib - CAS 1058156-90-3
Catalog number: B0084-474328
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C23H22FN3O3
Molecular Weight:
407.445
COA:
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Targets:
EGFR | VEGFR
Description:
Anlotibib is a multi-targetes kinase inhibitor of receptor tyrosine and could effectively resist the formation of new angiogenesis. It is undergoing a phase III clinical trial for therapy of metastatic or advanced alveolar soft part sarcoma (ASPS), leiomyosarcoma (LMS), and synovial sarcoma (SS).
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-474328 50 mg $228 In stock
B0084-474328 100 mg $398 In stock
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Purity:
>98%
Related CAS:
1360460-82-7 (hydrochloride)
Appearance:
Solid Powder
Synonyms:
1-[[4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-6-methoxyquinolin-7-yl]oxymethyl]cyclopropan-1-amine
Solubility:
Soluble to 44 mg/mL DMSO.
Storage:
Store at -20°C
MSDS:
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Shelf Life:
2 years
InChIKey:
KSMZEXLVHXZPEF-UHFFFAOYSA-N
InChI:
InChI=1S/C23H22FN3O3/c1-13-9-15-16(27-13)3-4-19(22(15)24)30-18-5-8-26-17-11-21(20(28-2)10-14(17)18)29-12-23(25)6-7-23/h3-5,8-11,27H,6-7,12,25H2,1-2H3
Canonical SMILES:
CC1=CC2=C(N1)C=CC(=C2F)OC3=C4C=C(C(=CC4=NC=C3)OCC5(CC5)N)OC
1.Influences of Anlotinib on Cytochrome P450 Enzymes in Rats Using a Cocktail Method.
Sun W;Wang Z;Chen R;Huang C;Sun R;Hu X;Li W;Chen R Biomed Res Int. 2017;2017:3619723. doi: 10.1155/2017/3619723. Epub 2017 Dec 26.
The present study aimed to investigate the effect of anlotinib (AL3818) on pharmacokinetics of cytochrome P450 (CYP) enzymes (CYP1A2, CYP2C6, CYP2D1, CYP2D2, and CYP3A1/2) by using five cocktail probe drugs in vivo. After pretreatment for 7 days with anlotinib (treatment group) or saline (control group) by oral administration, probe drugs phenacetin, tolbutamide, omeprazole, metoprolol, and midazolam were administered to rats by oral administration. Blood samples were obtained at a series of time-points and the concentrations of five probe drugs in plasma were determined by a UHPLC-MS/MS method. The results showed that treatment with anlotinib had no significant effect on rat CYP1A2, CYP2D2, and CYP2C6. However, anlotinib had a significant inductive effect on CYP2D1 and CYP3A1/2. Therefore, caution is needed during the concomitant use of anlotinib with other drugs metabolized by CYP2D1 and CYP3A1/2 because of potential drug-anlotinib interactions.
2.Safety and Efficacy of the S-1/Temozolomide Regimen in Patients with Metastatic Neuroendocrine Tumors.
Zhao J;Zhao H;Chi Y Neuroendocrinology. 2018;106(4):318-323. doi: 10.1159/000480402. Epub 2017 Aug 17.
PURPOSE: ;Both capecitabine alone and capecitabine in combination with temozolomide have activities against neuroendocrine tumors (NETs). However, the role of S-1 in NETs is still unknown. We performed a study to evaluate the safety and efficacy of the S-1/temozolomide (STEM) regimen in patients with locally advanced or metastatic NETs.;METHODS: ;A retrospective review was conducted in 20 patients with locally advanced or metastatic NETs treated with the STEM regimen. Of the patients, 15 (75.00%) had failed 1 or more lines of treatment with somatostatin analogues, sunitinib, everolimus, anlotinib, or other chemotherapy regimens. The patients received S-1 at 40 mg/m2 orally twice daily on days 1-14 and temozolomide 200 mg orally once daily on days 10-14 of a 21-day cycle. The patients were followed up for evidence of object response, toxicity, and progression-free survival.;RESULTS: ;Response to treatment was assessed using RECIST 1.1. Eight patients (40.00%) achieved a partial response (PR), and another 8 (40.00%) had stable disease (SD). The clinical benefit rate (PR and SD) was 80.00%. The median progression-free survival was not achieved. Only 1 patient (5.00%) had grade 3 adverse events.
3.Safety and Efficacy of Anlotinib, a Multikinase Angiogenesis Inhibitor, in Patients With Refractory Metastatic Soft Tissue Sarcoma.
Chi Y;Fang Z;Hong XN;Yao Y;Sun P;Wang G;Du F;Sun Y;Wu Q;Qu G;Wang S;Song J;Yu J;Lu Y;Zhu X;Niu X;He Z;Wang J;Yu H;Cai J Clin Cancer Res. 2018 Jun 12. pii: clincanres.3766.2017. doi: 10.1158/1078-0432.CCR-17-3766. [Epub ahead of print]
PURPOSE: ;The prognosis for patients with refractory soft-tissue sarcoma (STS) is dismal. Anlotinib has previously shown antitumor activity on STS in preclinical and phase I studies.;EXPERIMENTAL DESIGN: ;Patients 18 years and older, progressing after anthracycline-based chemotherapy, naïve from angiogenesis inhibitors, with at least one measurable lesion according to RECIST 1.1, were enrolled. The main subtypes eligible were: undifferentiated pleomorphic sarcoma (UPS), liposarcoma (LPS), leiomyosarcoma (LMS), synovial sarcoma (SS), fibrosarcoma (FS), alveolar soft part sarcoma (ASPS) and clear cell sarcoma (CCS). Participants were treated with anlotinib. The primary endpoint was progression-free rate at 12 weeks (PFR 12 weeks).;RESULTS: ;166 patients were included in the final analysis. Overall, the PFR 12 weeks was 68% and objective response rate was 13% (95% CI 7.6%-18%). The median progression free survival (PFS) and overall survival (OS) were 5.6 and 12 months respectively. The PFR 12 weeks, median PFS and OS were: 58%, 4.1 and 11 months for UPS (n=19); 63%, 5.6 and 13 months for LPS (n=13); 75%, 11 and 15 months for LMS (n=26); 75%, 7.7 and 12 months for SS (n=47); 81%, 5.6 and 12 months for FS (n=18); 77%, 21 and not reached for ASPS (n=13); 54%, 11 and 16 months for CCS (n=7); 44%, 2.
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