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商品详细MedKoo/Motesanibfeatured/10mg/201934
MedKoo/Motesanibfeatured/10mg/201934
MedKoo/Motesanibfeatured/10mg/201934
商品编号: 201934
品牌: MedKoo
市场价: ¥3000.00
美元价: 1800.00
产地: 美国(厂家直采)
公司:
产品分类: 多肽合成
公司分类: peptide
联系Q Q: 3392242852
电话号码: 4000-520-616
电子邮箱: info@ebiomall.com
商品介绍

Motesanib
featured

WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#:201934

CAS#:453562-69-1 (free base)

Description:Motesanib, also known as AMG-706, is the orally bioavailable multiple-receptor tyrosine kinase inhibitor with potential antineoplastic activity. Motesanib selectively targets and inhibits vascular endothelial growth factor (VEGFR), platelet-derived growth factor (PDGFR), kit, and Ret receptors, thereby inhibiting angiogenesis and cellular proliferation.

Price and Availability

SizePriceShipping out timeQuantity
10mgUSD 150Same Day
25mgUSD 250Same Day
50mgUSD 450Same Day
100mgUSD 650Same Day
200mgUSD 950Same Day
500mgUSD 1650Same Day
1gUSD 28502 Weeks
2gUSD 38502 Weeks
5gUSD 58502 Weeks
Inquire bulk and customized quantity

Pricing updated 2021-01-23.Prices are subject to change without notice.

Motesanib (free base), purity > 98%, is in stock. The same day shipping after order is received.

Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 201934Name: MotesanibCAS#: 453562-69-1 (free base)Chemical Formula: C22H23N5OExact Mass: 373.1902Molecular Weight: 373.46Elemental Analysis: C, 70.76; H, 6.21; N, 18.75; O, 4.28

Related CAS #:453562-69-1 (free base)857876-30-3 (phosphate)

Synonym:AMG 706; AMG706; AMG706; motesanib free base

IUPAC/Chemical Name:N-(3,3-dimethyl-2,3-dihydro-1H-indol-6-yl)-2-[(pyridin-4- ylmethyl)amino]pyridine-3-carboxamide

InChi Key:RAHBGWKEPAQNFF-UHFFFAOYSA-N

InChi Code:InChI=1S/C22H23N5O/c1-22(2)14-26-19-12-16(5-6-18(19)22)27-21(28)17-4-3-9-24-20(17)25-13-15-7-10-23-11-8-15/h3-12,26H,13-14H2,1-2H3,(H,24,25)(H,27,28)

SMILES Code:O=C(C1=CC=CN=C1NCC2=CC=NC=C2)NC3=CC4=C(C=C3)C(C)(C)CN4

Technical Data

Appearance:
White to off-white solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:
View CoA: current batch, Lot#CRB50713

QC Data:
View QC data: current batch, Lot#CRB50713

Safety Data Sheet (SDS):
View Safety Data Sheet (SDS)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001

Additional Information

Motesanib is an orally-administered small molecule antagonist of vascular endothelial growth factor receptors 1, 2 and 3 (“VEGFR1-3”), platelet-derived growth factor receptor (“PDGFR”) and stem cell factor receptor (“c-kit”). It is being investigated as a cancer treatment. We are developing this product in collaboration with Takeda.      

References

1: Kubota K, Yoshioka H, Oshita F, Hida T, Yoh K, Hayashi H, Kato T, Kaneda H, Yamada K, Tanaka H, Ichinose Y, Park K, Cho EK, Lee KH, Lin CB, Yang JC, Hara K,Asato T, Nakagawa K. Phase III, Randomized, Placebo-Controlled, Double-Blind Trial of Motesanib (AMG-706) in Combination With Paclitaxel and Carboplatin in East Asian Patients With Advanced Nonsquamous Non-Small-Cell Lung Cancer. J ClinOncol. 2017 Nov 10;35(32):3662-3670. doi: 10.1200/JCO.2017.72.7297. Epub 2017 Sep 13. PubMed PMID: 28902534.

2: Torok S, Rezeli M, Kelemen O, Vegvari A, Watanabe K, Sugihara Y, Tisza A, Marton T, Kovacs I, Tovari J, Laszlo V, Helbich TH, Hegedus B, Klikovits T, HodaMA, Klepetko W, Paku S, Marko-Varga G, Dome B. Limited Tumor Tissue Drug Penetration Contributes to Primary Resistance against Angiogenesis Inhibitors. Theranostics. 2017 Jan 1;7(2):400-412. doi: 10.7150/thno.16767. eCollection 2017. PubMed PMID: 28042343; PubMed Central PMCID: PMC5197073.

3: Skouras VS, Maragkos C, Grapsa D, Syrigos KN. Targeting Neovasculature with Multitargeted Antiangiogenesis Tyrosine Kinase Inhibitors in Non-small Cell LungCancer. BioDrugs. 2016 Oct;30(5):421-439. Review. PubMed PMID: 27670779.

4: Song J, Kim SB, Kim KH, Kim TN, Lee KH. A case report of motesanib-induced biliary sludge formation causing obstructive cholangitis with acute pancreatitistreated by endoscopic sphincterotomy. Medicine (Baltimore). 2016 Sep;95(37):e4645. doi: 10.1097/MD.0000000000004645. PubMed PMID: 27631212; PubMed Central PMCID: PMC5402555.

5: Yamauchi F, Kamioka Y, Yano T, Matsuda M. In Vivo FRET Imaging of Tumor Endothelial Cells Highlights a Role of Low PKA Activity in Vascular Hyperpermeability. Cancer Res. 2016 Sep 15;76(18):5266-76. doi: 10.1158/0008-5472.CAN-15-3534. Epub 2016 Aug 3. PubMed PMID: 27488524.

6: Gosselin NH, Mouksassi MS, Lu JF, Hsu CP. Population pharmacokinetic modelingof motesanib and its active metabolite, M4, in cancer patients. Clin Pharmacol Drug Dev. 2015 Nov;4(6):463-72. doi: 10.1002/cpdd.196. Epub 2015 Jul 23. PubMed PMID: 27137719.

7: Kaya TT, Altun A, Turgut NH, Ataseven H, Koyluoglu G. Effects of a Multikinase Inhibitor Motesanib (AMG 706) Alone and Combined with the Selective DuP-697 COX-2 Inhibitor on Colorectal Cancer Cells. Asian Pac J Cancer Prev. 2016;17(3):1103-10. PubMed PMID: 27039732.

8: Tarshis S, Maltzahn J, Loomis Z, Irwin DC. Preventing High Altitude Cerebral Edema in Rats with Repurposed Anti-Angiogenesis Pharmacotherapy. Aerosp Med Hum Perform. 2016 Dec 1;87(12):1031-1035. doi: 10.3357/AMHP.4571.2016. PubMed PMID: 28323589.

9: Dunna NR, Kandula V, Girdhar A, Pudutha A, Hussain T, Bandaru S, Nayarisseri A. High Affinity Pharmacological Profiling of Dual Inhibitors Targeting RET and VEGFR2 in Inhibition of Kinase and Angiogeneis Events in Medullary Thyroid Carcinoma. Asian Pac J Cancer Prev. 2015;16(16):7089-95. PubMed PMID: 26514495.

10: Gao C, Grøtli M, Eriksson LA. Characterization of interactions and pharmacophore development for DFG-out inhibitors to RET tyrosine kinase. J Mol Model. 2015 Jul;21(7):167. doi: 10.1007/s00894-015-2708-z. Epub 2015 Jun 6. PubMed PMID: 26044359.

11: Caglevic C, Grassi M, Raez L, Listi A, Giallombardo M, Bustamante E, Gil-Bazo I, Rolfo C. Nintedanib in non-small cell lung cancer: from preclinical to approval. Ther Adv Respir Dis. 2015 Aug;9(4):164-72. doi: 10.1177/1753465815579608. Epub 2015 Apr 7. Review. PubMed PMID: 25855060.

12: PLOS ONE Staff. Correction: challenges in developing a validated biomarker for angiogenesis inhibitors: the motesanib experience. PLoS One. 2015 Mar 26;10(3):e0121162. doi: 10.1371/journal.pone.0121162. eCollection 2015. PubMed PMID: 25811784; PubMed Central PMCID: PMC4374716.

13: Tebbutt N, Kotasek D, Burris HA, Schwartzberg LS, Hurwitz H, Stephenson J, Warner DJ, Chen L, Hsu CP, Goldstein D. Motesanib with or without panitumumab plus FOLFIRI or FOLFOX for the treatment of metastatic colorectal cancer. CancerChemother Pharmacol. 2015 May;75(5):993-1004. doi: 10.1007/s00280-015-2694-y. Epub 2015 Mar 15. PubMed PMID: 25772756.

14: Greenall SA, Donoghue JF, Van Sinderen M, Dubljevic V, Budiman S, Devlin M, Street I, Adams TE, Johns TG. EGFRvIII-mediated transactivation of receptor tyrosine kinases in glioma: mechanism and therapeutic implications. Oncogene. 2015 Oct 8;34(41):5277-87. doi: 10.1038/onc.2014.448. Epub 2015 Feb 9. PubMed PMID: 25659577.

15: Gruber JJ, Colevas AD. Differentiated thyroid cancer: focus on emerging treatments for radioactive iodine-refractory patients. Oncologist. 2015 Feb;20(2):113-26. doi: 10.1634/theoncologist.2014-0313. Epub 2015 Jan 23. Review. PubMed PMID: 25616432; PubMed Central PMCID: PMC4319630.

16: Lkhoyaali S, Benhmida S, Ait Elhaj M, Layachi M, Bensouda Y, Errihani H. [Targeted therapy in thyroid cancer: Towards a treatment card]. Pathol Biol (Paris). 2015 Feb;63(1):1-6. doi: 10.1016/j.patbio.2014.11.003. Epub 2014 Dec 30. Review. French. PubMed PMID: 25555494.

17: Hong DS, Kurzrock R, Mulay M, Rasmussen E, Wu BM, Bass MB, Zhong ZD, FribergG, Rosen LS. A phase 1b, open-label study of trebananib plus bevacizumab or motesanib in patients with solid tumours. Oncotarget. 2014 Nov 30;5(22):11154-67. PubMed PMID: 25525888; PubMed Central PMCID: PMC4294348.

18: Bass MB, Yao B, Hei YJ, Ye Y, Davis GJ, Davis MT, Kaesdorf BA, Chan SS, Patterson SD. Challenges in developing a validated biomarker for angiogenesis inhibitors: the motesanib experience. PLoS One. 2014 Oct 14;9(10):e108048. doi: 10.1371/journal.pone.0108048. eCollection 2014. Erratum in: PLoS One. 2015;10(3):e0121162. PubMed PMID: 25314641; PubMed Central PMCID: PMC4196848.

19: Kim JG. Molecular pathogenesis and targeted therapies in well-differentiatedthyroid carcinoma. Endocrinol Metab (Seoul). 2014 Sep;29(3):211-6. doi: 10.3803/EnM.2014.29.3.211. Review. PubMed PMID: 25309777; PubMed Central PMCID: PMC4192816.

20: Wang YJ, Zhang YK, Kathawala RJ, Chen ZS. Repositioning of Tyrosine Kinase Inhibitors as Antagonists of ATP-Binding Cassette Transporters in Anticancer Drug Resistance. Cancers (Basel). 2014 Sep 29;6(4):1925-52. doi: 10.3390/cancers6041925. Review. PubMed PMID: 25268163; PubMed Central PMCID: PMC4276951.

品牌介绍
MedKoo 美帝药库公司以药物化学合成技术为核心,密切结合全球抗癌新药研发领域中的新技术、新理论、新趋势和新的发展方向,不断推出抗癌化合物新品种。 。 美帝药库MedKoo将在中国建立药物化学合成生产基地和多个现代化药物化合物存储仓库。 美帝药库的药物化合物来源于以下几个渠道:自主合成、委托化学合成、合作伙伴、和从国内外市场上选购。 MedKoo美帝药库的抗癌分子库 MedKoo的目标是打造全球规模最大、品种最多、类别最全和质量最好的小分子抗癌化合物库。MedKoo的抗癌药库将由下列5个分子库组成: (1)上市抗癌药库:该库将含有大约100个全球已批准上市的小分子抗癌化合物; (2)抗癌候选药物库:该分子库含有大约400个世界各国正在临床研究中抗癌小分子候选药物; (3)同系抗癌分子库:该分子库将含有多个化学结构类似或抗癌机制类似的分子包; (4)抗癌分子预制模块库:该库主要含有用于组建抗癌目标分子的分子模块包; (5)同位素标记抗癌分子库。