Capmatinib
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MedKoo CAT#: 205494

CAS#: 1029712-80-8 (free base)

Description: Capmatinib, also known as INCB28060 and INC280, is an orally bioavailable inhibitor of the proto-oncogene c-Met (hepatocyte growth factor receptor [HGFR]) with potential antineoplastic activity. c-Met inhibitor INC280 selectively binds to c-Met, thereby inhibiting c-Met phosphorylation and disrupting c-Met signal transduction pathways. This may induce cell death in tumor cells overexpressing c-Met protein or expressing constitutively activated c-Met protein. Capmatinib was approved in 2020.


Price and Availability

Size Price Shipping out time Quantity
100mg USD 90 Same day
200mg USD 150 Same day
500mg USD 250 Same day
1g USD 450 Same day
2g USD 650 Same day
5g USD 1450 Same day
10g USD 2550 Same day
20g USD 4550 Same day
Inquire bulk and customized quantity

Pricing updated 2020-10-20. Prices are subject to change without notice.

Capmatinib, purity > 98%, is in stock. The same day shipping out after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 205494
Name: Capmatinib
CAS#: 1029712-80-8 (free base)
Chemical Formula: C23H17FN6O
Exact Mass: 412.14479
Molecular Weight: 412.42
Elemental Analysis: C, 66.98; H, 4.15; F, 4.61; N, 20.38; O, 3.88


Related CAS #: 1029712-80-8 (free base)   1865733-40-9 (HCl hydrate)   1029714-89-3 (xHCl)   1197376-85-4 (2HCl)   1197376-90-1 (besylate)   1450883-33-6 (fumarate)    

Synonym: INC280; INC-280; INC 280; INCB028060; INCB-028060; INCB 028060; INCB28060; INCB-28060; INCB 28060; Capmatinib.

IUPAC/Chemical Name: 2-fluoro-N-methyl-4-(7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl)benzamide

InChi Key: LIOLIMKSCNQPLV-UHFFFAOYSA-N

InChi Code: InChI=1S/C23H17FN6O/c1-25-22(31)18-6-5-16(11-19(18)24)21-13-28-23-27-12-17(30(23)29-21)10-14-4-7-20-15(9-14)3-2-8-26-20/h2-9,11-13H,10H2,1H3,(H,25,31)

SMILES Code: O=C(NC)C1=CC=C(C2=NN3C(N=C2)=NC=C3CC4=CC=C5N=CC=CC5=C4)C=C1F


Technical Data

Appearance:
Yellow solid powder

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

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

INCB28060 exhibits picomolar enzymatic potency and is highly specific for c-MET with more than 10,000-fold selectivity over a large panel of human kinases. This inhibitor potently blocks c-MET phosphorylation and activation of its key downstream effectors in c-MET-dependent tumor cell lines. As a result, INCB28060 potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis in vitro. Oral dosing of INCB28060 results in time- and dose-dependent inhibition of c-MET phosphorylation and tumor growth in c-MET-driven mouse tumor models, and the inhibitor is well tolerated at doses that achieve complete tumor inhibition. In a further exploration of potential interactions between c-MET and other signaling pathways, we found that activated c-MET positively regulates the activity of epidermal growth factor receptors (EGFR) and HER-3, as well as expression of their ligands. These effects are reversed with INCB28060 treatment. Finally, we confirmed that circulating hepatocyte growth factor levels are significantly elevated in patients with various cancers. Activated c-MET has pleiotropic effects on multiple cancer-promoting signaling pathways and may play a critical role in driving tumor cell growth and survival. INCB28060 is a potent and selective c-MET kinase inhibitor that may have therapeutic potential in cancer treatment. (source: Clin Cancer Res; 17(22); 7127-38. ©2011 AACR.)
  
 
 


References

1: Vansteenkiste JF, Van De Kerkhove C, Wauters E, Van Mol P. Capmatinib for the treatment of non-small cell lung cancer. Expert Rev Anticancer Ther. 2019 Aug;19(8):659-671. doi: 10.1080/14737140.2019.1643239. Epub 2019 Aug 1. PMID: 31368815.

2: Wu YL, Zhang L, Kim DW, Liu X, Lee DH, Yang JC, Ahn MJ, Vansteenkiste JF, Su WC, Felip E, Chia V, Glaser S, Pultar P, Zhao S, Peng B, Akimov M, Tan DSW. Phase Ib/II Study of Capmatinib (INC280) Plus Gefitinib After Failure of Epidermal Growth Factor Receptor (EGFR) Inhibitor Therapy in Patients With EGFR- Mutated, MET Factor-Dysregulated Non-Small-Cell Lung Cancer. J Clin Oncol. 2018 Nov 1;36(31):3101-3109. doi: 10.1200/JCO.2018.77.7326. Epub 2018 Aug 29. Erratum in: J Clin Oncol. 2019 Jan 20;37(3):261. PMID: 30156984.

3: Baltschukat S, Engstler BS, Huang A, Hao HX, Tam A, Wang HQ, Liang J, DiMare MT, Bhang HC, Wang Y, Furet P, Sellers WR, Hofmann F, Schoepfer J, Tiedt R. Capmatinib (INC280) Is Active Against Models of Non-Small Cell Lung Cancer and Other Cancer Types with Defined Mechanisms of MET Activation. Clin Cancer Res. 2019 May 15;25(10):3164-3175. doi: 10.1158/1078-0432.CCR-18-2814. Epub 2019 Jan 23. PMID: 30674502.

4: Capmatinib Triggers Responses in NSCLC. Cancer Discov. 2019 Jan;9(1):OF6. doi: 10.1158/2159-8290.CD-NB2018-148. Epub 2018 Nov 14. PMID: 30429129.

5: Esaki T, Hirai F, Makiyama A, Seto T, Bando H, Naito Y, Yoh K, Ishihara K, Kakizume T, Natsume K, Myers A, Doi T. Phase I dose-escalation study of capmatinib (INC280) in Japanese patients with advanced solid tumors. Cancer Sci. 2019 Apr;110(4):1340-1351. doi: 10.1111/cas.13956. Epub 2019 Feb 20. PMID: 30724423; PMCID: PMC6447844.

6: Ko B, Halmos B. Capmatinib and gefitinib combination therapy: will EGFR- mutated MET-dysregulated NSCLC "capitulate"? Transl Lung Cancer Res. 2018 Dec;7(Suppl 4):S321-S325. doi: 10.21037/tlcr.2018.12.05. PMID: 30705845; PMCID: PMC6328688.

7: Kim S, Kim TM, Kim DW, Kim S, Kim M, Ahn YO, Keam B, Heo DS. Acquired Resistance of MET-Amplified Non-small Cell Lung Cancer Cells to the MET Inhibitor Capmatinib. Cancer Res Treat. 2019 Jul;51(3):951-962. doi: 10.4143/crt.2018.052. Epub 2018 Oct 10. PMID: 30309221; PMCID: PMC6639226.

8: Dhillon S. Capmatinib: First Approval. Drugs. 2020 Jul;80(11):1125-1131. doi: 10.1007/s40265-020-01347-3. PMID: 32557339.

9: Capmatinib Could Alter NSCLC Treatment Landscape. Cancer Discov. 2020 Jun;10(6):OF4. doi: 10.1158/2159-8290.CD-NB2020-038. Epub 2020 Apr 29. PMID: 32349974.

10: Burki TK. Preliminary activity of capmatinib with gefitinib in NSCLC. Lancet Oncol. 2018 Oct;19(10):e517. doi: 10.1016/S1470-2045(18)30678-8. Epub 2018 Sep 6. PMID: 30197173.

11: Bang YJ, Su WC, Schuler M, Nam DH, Lim WT, Bauer TM, Azaro A, Poon RTP, Hong D, Lin CC, Akimov M, Ghebremariam S, Zhao S, Giovannini M, Ma B. Phase 1 study of capmatinib in MET-positive solid tumor patients: Dose escalation and expansion of selected cohorts. Cancer Sci. 2020 Feb;111(2):536-547. doi: 10.1111/cas.14254. Epub 2019 Dec 30. PMID: 31778267; PMCID: PMC7004521.

12: Qin S, Chan SL, Sukeepaisarnjaroen W, Han G, Choo SP, Sriuranpong V, Pan H, Yau T, Guo Y, Chen M, Ren Z, Xu J, Yen CJ, Lin ZZ, Manenti L, Gu Y, Sun Y, Tiedt R, Hao L, Song W, Tanwandee T. A phase II study of the efficacy and safety of the MET inhibitor capmatinib (INC280) in patients with advanced hepatocellular carcinoma. Ther Adv Med Oncol. 2019 Dec 11;11:1758835919889001. doi: 10.1177/1758835919889001. Erratum in: Ther Adv Med Oncol. 2020 Mar 12;12:1758835920913426. PMID: 31853265; PMCID: PMC6906348.

13: Going After METex14 in NSCLC. Cancer Discov. 2019 Aug;9(8):OF9. doi: 10.1158/2159-8290.CD-ND2019-006. Epub 2019 Jun 17. PMID: 31209157.

14: Shaker ME, Ashamallah SA, El-Mesery M. The novel c-Met inhibitor capmatinib mitigates diethylnitrosamine acute liver injury in mice. Toxicol Lett. 2016 Nov 2;261:13-25. doi: 10.1016/j.toxlet.2016.08.015. Epub 2016 Aug 21. PMID: 27553677.

15: Bouattour M, Raymond E, Qin S, Cheng AL, Stammberger U, Locatelli G, Faivre S. Recent developments of c-Met as a therapeutic target in hepatocellular carcinoma. Hepatology. 2018 Mar;67(3):1132-1149. doi: 10.1002/hep.29496. Epub 2018 Feb 1. PMID: 28862760; PMCID: PMC5873445.

16: Li H, Li CW, Li X, Ding Q, Guo L, Liu S, Liu C, Lai CC, Hsu JM, Dong Q, Xia W, Hsu JL, Yamaguchi H, Du Y, Lai YJ, Sun X, Koller PB, Ye Q, Hung MC. MET Inhibitors Promote Liver Tumor Evasion of the Immune Response by Stabilizing PDL1. Gastroenterology. 2019 May;156(6):1849-1861.e13. doi: 10.1053/j.gastro.2019.01.252. Epub 2019 Jan 31. PMID: 30711629; PMCID: PMC6904924.

17: Saad KM, Shaker ME, Shaaban AA, Abdelrahman RS, Said E. The c-Met inhibitor capmatinib alleviates acetaminophen-induced hepatotoxicity. Int Immunopharmacol. 2020 Apr;81:106292. doi: 10.1016/j.intimp.2020.106292. Epub 2020 Feb 14. PMID: 32062076.

18: Reungwetwattana T, Liang Y, Zhu V, Ou SI. The race to target MET exon 14 skipping alterations in non-small cell lung cancer: The Why, the How, the Who, the Unknown, and the Inevitable. Lung Cancer. 2017 Jan;103:27-37. doi: 10.1016/j.lungcan.2016.11.011. Epub 2016 Nov 15. PMID: 28024693.

19: Gautschi O, Menon R, Bertrand M, Murer C, Diebold J. Capmatinib and Osimertinib Combination Therapy for EGFR-Mutant Lung Adenocarcinoma. J Thorac Oncol. 2020 Jan;15(1):e13-e15. doi: 10.1016/j.jtho.2019.07.027. PMID: 31864554.

20: Schuler M, Berardi R, Lim WT, de Jonge M, Bauer TM, Azaro A, Gottfried M, Han JY, Lee DH, Wollner M, Hong DS, Vogel A, Delmonte A, Akimov M, Ghebremariam S, Cui X, Nwana N, Giovannini M, Kim TM. Molecular correlates of response to capmatinib in advanced non-small-cell lung cancer: clinical and biomarker results from a phase I trial. Ann Oncol. 2020 Mar 30:S0923-7534(20)36380-8. doi: 10.1016/j.annonc.2020.03.293. Epub ahead of print. PMID: 32240796.