XMD8-92
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 407373

CAS#: 1234480-50-2

Description: XMD8-92 is a BMK1 inhibitor and a highly selective inhibitor of ERK5 activity. XMD8-92 inhibits pancreatic tumor xenograft growth via a DCLK1-dependent mechanism. XMD8-92 blocks cellular BMK1 activation and significantly suppresses tumor growth in lung and cervical tumor models and is well tolerated in animals.


Price and Availability

Size
Price

100mg
USD 550
1g
USD 2950
Size
Price

200mg
USD 950
2g
USD 4450
Size
Price

500mg
USD 1850
5g
USD 7650

XMD8-92, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received. Delivery time: overnight (USA/Canada); 3-5 days (worldwide).


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 407373
Name: XMD8-92
CAS#: 1234480-50-2
Chemical Formula: C26H30N6O3
Exact Mass: 474.2379
Molecular Weight: 474.565
Elemental Analysis: C, 65.80; H, 6.37; N, 17.71; O, 10.11


Synonym: XMD8-92; XMD-8-92; XMD 8-92; XMD892; XMD-892; XMD 892.

IUPAC/Chemical Name: 2-[[2-ethoxy-4-(4-hydroxy-1-piperidinyl)phenyl]amino]-5,11-dihydro-5,11-dimethyl-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one

InChi Key: QAPAJIZPZGWAND-UHFFFAOYSA-N

InChi Code: InChI=1S/C26H30N6O3/c1-4-35-23-15-17(32-13-11-18(33)12-14-32)9-10-20(23)28-26-27-16-22-24(29-26)30(2)21-8-6-5-7-19(21)25(34)31(22)3/h5-10,15-16,18,33H,4,11-14H2,1-3H3,(H,27,28,29)

SMILES Code: O=C1N(C)C2=CN=C(NC3=CC=C(N4CCC(O)CC4)C=C3OCC)N=C2N(C)C5=CC=CC=C15


Technical Data

Appearance:
White to beige solid powder.

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

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

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).

Harmonized System Code:
293490


References

1: Sureban SM, May R, Weygant N, Qu D, Chandrakesan P, Bannerman-Menson E, Ali N, Pantazis P, Westphalen CB, Wang TC, Houchen CW. XMD8-92 inhibits pancreatic tumor xenograft growth via a DCLK1-dependent mechanism. Cancer Lett. 2014 Aug 28;351(1):151-61. doi: 10.1016/j.canlet.2014.05.011. PubMed PMID: 24880079.

2: Song C, Xu Q, Jiang K, Zhou G, Yu X, Wang L, Zhu Y, Fang L, Yu Z, Lee JD, Yu SC, Yang Q. Inhibition of BMK1 pathway suppresses cancer stem cells through BNIP3 and BNIP3L. Oncotarget. 2015 Oct 20;6(32):33279-89. doi: 10.18632/oncotarget.5337. PubMed PMID: 26432836; PubMed Central PMCID: PMC4741765.

3: Bo Z, Bin G, Jing W, Cuifang W, Liping A, Jinglin M, Jin J, Xiaoyi T, Cong C, Ning D, Yayi X. Fluid shear stress promotes osteoblast proliferation via the Gαq-ERK5 signaling pathway. Connect Tissue Res. 2016 Jul;57(4):299-306. doi: 10.1080/03008207.2016.1181063. PubMed PMID: 27115838.

4: Wang J, Li Q, Wang C, Xiong Q, Lin Y, Sun Q, Jin H, Yang F, Ren X, Pang T. Knock-down of CIAPIN1 sensitizes K562 chronic myeloid leukemia cells to Imatinib by regulation of cell cycle and apoptosis-associated members via NF-κB and ERK5 signaling pathway. Biochem Pharmacol. 2016 Jan 1;99:132-45. doi: 10.1016/j.bcp.2015.12.002. PubMed PMID: 26679828.

5: Rovida E, Di Maira G, Tusa I, Cannito S, Paternostro C, Navari N, Vivoli E, Deng X, Gray NS, Esparís-Ogando A, David E, Pandiella A, Dello Sbarba P, Parola M, Marra F. The mitogen-activated protein kinase ERK5 regulates the development and growth of hepatocellular carcinoma. Gut. 2015 Sep;64(9):1454-65. doi: 10.1136/gutjnl-2014-306761. PubMed PMID: 25183205.

6: Wang X, Pesakhov S, Harrison JS, Danilenko M, Studzinski GP. ERK5 pathway regulates transcription factors important for monocytic differentiation of human myeloid leukemia cells. J Cell Physiol. 2014 Jul;229(7):856-67. doi: 10.1002/jcp.24513. PubMed PMID: 24264602; PubMed Central PMCID: PMC4363988.

7: Yang Q, Lee JD. Targeting the BMK1 MAP kinase pathway in cancer therapy. Clin Cancer Res. 2011 Jun 1;17(11):3527-32. doi: 10.1158/1078-0432.CCR-10-2504. PubMed PMID: 21385929; PubMed Central PMCID: PMC3107913.

8: Zheng R, Studzinski GP. Optimal AraC-Cytotoxicity to AML Cells Requires ERK5 Activity. J Cell Biochem. 2016 Dec 6. doi: 10.1002/jcb.25820. [Epub ahead of print] PubMed PMID: 27922189.

9: Park SJ, Choi YS, Lee S, Lee YJ, Hong S, Han S, Kim BC. BIX02189 inhibits TGF-β1-induced lung cancer cell metastasis by directly targeting TGF-β type I receptor. Cancer Lett. 2016 Oct 28;381(2):314-22. doi: 10.1016/j.canlet.2016.08.010. PubMed PMID: 27543359.

10: Bin G, Cuifang W, Bo Z, Jing W, Jin J, Xiaoyi T, Cong C, Yonggang C, Liping A, Jinglin M, Yayi X. Fluid shear stress inhibits TNF-α-induced osteoblast apoptosis via ERK5 signaling pathway. Biochem Biophys Res Commun. 2015 Oct 9;466(1):117-23. doi: 10.1016/j.bbrc.2015.08.117. PubMed PMID: 26325467.

11: Wang X, Pesakhov S, Weng A, Kafka M, Gocek E, Nguyen M, Harrison JS, Danilenko M, Studzinski GP. ERK 5/MAPK pathway has a major role in 1α,25-(OH)2 vitamin D3-induced terminal differentiation of myeloid leukemia cells. J Steroid Biochem Mol Biol. 2014 Oct;144 Pt A:223-7. doi: 10.1016/j.jsbmb.2013.10.002. Review. PubMed PMID: 24514755; PubMed Central PMCID: PMC4000286.

12: Bera A, Das F, Ghosh-Choudhury N, Li X, Pal S, Gorin Y, Kasinath BS, Abboud HE, Ghosh Choudhury G. A positive feedback loop involving Erk5 and Akt turns on mesangial cell proliferation in response to PDGF. Am J Physiol Cell Physiol. 2014 Jun 1;306(11):C1089-100. doi: 10.1152/ajpcell.00387.2013. PubMed PMID: 24740537; PubMed Central PMCID: PMC4042091.

13: Amano S, Chang YT, Fukui Y. ERK5 activation is essential for osteoclast differentiation. PLoS One. 2015 Apr 17;10(4):e0125054. doi: 10.1371/journal.pone.0125054. PubMed PMID: 25885811; PubMed Central PMCID: PMC4401765.

14: Yang Q, Deng X, Lu B, Cameron M, Fearns C, Patricelli MP, Yates JR 3rd, Gray NS, Lee JD. Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein. Cancer Cell. 2010 Sep 14;18(3):258-67. doi: 10.1016/j.ccr.2010.08.008. Erratum in: Cancer Cell. 2010 Oct 19;18(4):396. PubMed PMID: 20832753; PubMed Central PMCID: PMC2939729.

15: Li Q, Chen Y, Zhang X, Zuo S, Ge H, Chen Y, Liu X, Zhang JH, Ruan H, Feng H. Scutellarin attenuates vasospasm through the Erk5-KLF2-eNOS pathway after subarachnoid hemorrhage in rats. J Clin Neurosci. 2016 Dec;34:264-270. doi: 10.1016/j.jocn.2016.09.028. PubMed PMID: 27742373.

16: Pereira DM, Simões AE, Gomes SE, Castro RE, Carvalho T, Rodrigues CM, Borralho PM. MEK5/ERK5 signaling inhibition increases colon cancer cell sensitivity to 5-fluorouracil through a p53-dependent mechanism. Oncotarget. 2016 Jun 7;7(23):34322-40. doi: 10.18632/oncotarget.9107. PubMed PMID: 27144434; PubMed Central PMCID: PMC5085159.

17: Ahmad R, Shihab PK, Jasem S, Behbehani K. FSL-1 induces MMP-9 production through TLR-2 and NF-κB /AP-1 signaling pathways in monocytic THP-1 cells. Cell Physiol Biochem. 2014;34(3):929-42. doi: 10.1159/000366310. PubMed PMID: 25200491.

18: Dong H, Liu Y, Zou Y, Li C, Li L, Li X, Zhao X, Zhou L, Liu J, Niu Y. Alteration of the ERK5 pathway by hydroxysafflor yellow A blocks expression of MEF2C in activated hepatic stellate cells in vitro: Potential treatment for hepatic fibrogenesis. Pharm Biol. 2013 Nov 5. [Epub ahead of print] PubMed PMID: 24192313.