NSC 42834 | CAS#195371-52-9 | JAK2 Inhibitor

MedKoo Cat#: 530455 | Name: NSC-42834

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Description:

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

NSC 42834, also known as JAK2 Inhibitor V, is an inhibitor of the autophosphorylation of wild type and V617F mutant forms of JAK2, displaying IC50 values between 10 and 30 µM.

Chemical Structure

NSC-42834

CAS#195371-52-9

Theoretical Analysis

MedKoo Cat#: 530455

Name: NSC-42834

CAS#: 195371-52-9

Chemical Formula: C23H24N2O

Exact Mass: 344.1889

Molecular Weight: 344.46

Elemental Analysis: C, 80.20; H, 7.02; N, 8.13; O, 4.64

Price and Availability

Size	Price	Availability
10mg	USD 300.00	2 Weeks
25mg	USD 550.00	2 Weeks
50mg	USD 950.00	2 Weeks
100mg	USD 1,650.00	2 Weeks

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Synonym

NSC 42834; NSC-42834; NSC42834; Janus-Associated Kinase Inhibitor V; Z3. JAK2 Inhibitor V.

IUPAC/Chemical Name

2-methyl-1-phenyl-4-(pyridin-2-yl)-2-(2-(pyridin-2-yl)ethyl)butan-1-one

InChi Key

SETYDCSRABYHSW-UHFFFAOYSA-N

InChi Code

InChI=1S/C23H24N2O/c1-23(15-13-20-11-5-7-17-24-20,16-14-21-12-6-8-18-25-21)22(26)19-9-3-2-4-10-19/h2-12,17-18H,13-16H2,1H3

SMILES Code

O=C(C(CCC1=CC=CC=N1)(CCC2=NC=CC=C2)C)C3=CC=CC=C3

Appearance

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).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

NSC 42834 (JAK2 Inhibitor V), a novel specific inhibitor of Jak2, inhibits Jak2-V617F and Jak2-WT autophosphorylation.

In vitro activity:

Z3 inhibited Jak2-V617F and Jak2-WT autophosphorylation in a dose-dependent manner but was not cytotoxic to cells at concentrations that inhibited kinase activity. Z3 selectively inhibited Jak2 kinase function with no effect on Tyk2 or c-Src kinase function. Z3 significantly inhibited proliferation of the Jak2-V617F-expressing, human erythroleukemia cell line, HEL 92.1.7. The Z3-mediated reduction in cell proliferation correlated with reduced Jak2 and STAT3 tyrosine phosphorylation levels as well as marked cell cycle arrest. Reference: Mol Cancer Ther. 2008 Aug;7(8):2308-18. https://pubmed.ncbi.nlm.nih.gov/18723478/

In vivo activity:

TBD

	Solvent	mg/mL	mM
Solubility
	DMF	30.0	87.09
	DMSO	60.0	174.19
	Ethanol	65.0	188.70
	Ethanol:PBS (pH 7.2) (1:1)	0.5	1.45

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 344.46 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

Sayyah J, Magis A, Ostrov DA, Allan RW, Braylan RC, Sayeski PP. Z3, a novel Jak2 tyrosine kinase small-molecule inhibitor that suppresses Jak2-mediated pathologic cell growth. Mol Cancer Ther. 2008 Aug;7(8):2308-18. doi: 10.1158/1535-7163.MCT-08-0279. PMID: 18723478; PMCID: PMC2579271.

In vitro protocol:

In vivo protocol:

TBD

1: Zhao C, Yang SH, Khadka DB, Jin Y, Lee KT, Cho WJ. Computer-aided discovery of aminopyridines as novel JAK2 inhibitors. Bioorg Med Chem. 2015 Mar 1;23(5):985-95. doi: 10.1016/j.bmc.2015.01.016. PubMed PMID: 25650310. 2: Sparidans RW, Durmus S, Xu N, Schinkel AH, Schellens JH, Beijnen JH. Liquid chromatography-tandem mass spectrometric assay for the JAK2 inhibitor CYT387 in plasma. J Chromatogr B Analyt Technol Biomed Life Sci. 2012 May 1;895-896:174-7. doi: 10.1016/j.jchromb.2012.03.021. PubMed PMID: 22476054. 3: Lin KL, Su JC, Chien CM, Chuang PW, Chang LS, Lin SR. Down-regulation of the JAK2/PI3K-mediated signaling activation is involved in Taiwan cobra cardiotoxin III-induced apoptosis of human breast MDA-MB-231 cancer cells. Toxicon. 2010 Jun 15;55(7):1263-73. doi: 10.1016/j.toxicon.2010.01.017. PubMed PMID: 20144642. 4: Tong H, Ren Y, Zhang F, Jin J. Homoharringtonine affects the JAK2-STAT5 signal pathway through alteration of protein tyrosine kinase phosphorylation in acute myeloid leukemia cells. Eur J Haematol. 2008 Oct;81(4):259-66. doi: 10.1111/j.1600-0609.2008.01116.x. PubMed PMID: 18616510. 5: Ren YL, Tong HY. [Effect of homoharringtonine combined with AG490 on JAK2-STAT5 associated signal pathway in HEL cells]. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2011 Oct;19(5):1117-20. Chinese. PubMed PMID: 22040954. 6: Szymańska J, Smolewski P, Majchrzak A, Cebula-Obrzut B, Chojnowski K, Treliński J. Pro-Apoptotic Activity of Ruxolitinib Alone and in Combination with Hydroxyurea, Busulphan, and PI3K/mTOR Inhibitors in JAK2-Positive Human Cell Lines. Adv Clin Exp Med. 2015 Mar-Apr;24(2):195-202. doi: 10.17219/acem/32934. PubMed PMID: 25931349. 7: Parada E, Egea J, Romero A, del Barrio L, García AG, López MG. Poststress treatment with PNU282987 can rescue SH-SY5Y cells undergoing apoptosis via α7 nicotinic receptors linked to a Jak2/Akt/HO-1 signaling pathway. Free Radic Biol Med. 2010 Dec 1;49(11):1815-21. doi: 10.1016/j.freeradbiomed.2010.09.017. PubMed PMID: 20875851. 8: Gross ER, Hsu AK, Gross GJ. The JAK/STAT pathway is essential for opioid-induced cardioprotection: JAK2 as a mediator of STAT3, Akt, and GSK-3 beta. Am J Physiol Heart Circ Physiol. 2006 Aug;291(2):H827-34. PubMed PMID: 16517948. 9: Lee JH, Park KS, Alberobello AT, Kallakury B, Weng MT, Wang Y, Giaccone G. The Janus kinases inhibitor AZD1480 attenuates growth of small cell lung cancers in vitro and in vivo. Clin Cancer Res. 2013 Dec 15;19(24):6777-86. doi: 10.1158/1078-0432.CCR-13-1110. PubMed PMID: 24158701; PubMed Central PMCID: PMC3872034. 10: Mathur A, Mo JR, Kraus M, O'Hare E, Sinclair P, Young J, Zhao S, Wang Y, Kopinja J, Qu X, Reilly J, Walker D, Xu L, Aleksandrowicz D, Marshall G, Scott ML, Kohl NE, Bachman E. An inhibitor of Janus kinase 2 prevents polycythemia in mice. Biochem Pharmacol. 2009 Aug 15;78(4):382-9. doi: 10.1016/j.bcp.2009.04.025. PubMed PMID: 19413997. 11: Ruchatz H, Coluccia AM, Stano P, Marchesi E, Gambacorti-Passerini C. Constitutive activation of Jak2 contributes to proliferation and resistance to apoptosis in NPM/ALK-transformed cells. Exp Hematol. 2003 Apr;31(4):309-15. PubMed PMID: 12691918. 12: Manshouri T, Quintás-Cardama A, Nussenzveig RH, Gaikwad A, Estrov Z, Prchal J, Cortes JE, Kantarjian HM, Verstovsek S. The JAK kinase inhibitor CP-690,550 suppresses the growth of human polycythemia vera cells carrying the JAK2V617F mutation. Cancer Sci. 2008 Jun;99(6):1265-73. doi: 10.1111/j.1349-7006.2008.00817.x. PubMed PMID: 18482053; PubMed Central PMCID: PMC4829954. 13: Iwamoto T, Senga T, Naito Y, Matsuda S, Miyake Y, Yoshimura A, Hamaguchi M. The JAK-inhibitor, JAB/SOCS-1 selectively inhibits cytokine-induced, but not v-Src induced JAK-STAT activation. Oncogene. 2000 Sep 28;19(41):4795-801. PubMed PMID: 11032030. 14: Sun J, Blaskovich MA, Jove R, Livingston SK, Coppola D, Sebti SM. Cucurbitacin Q: a selective STAT3 activation inhibitor with potent antitumor activity. Oncogene. 2005 May 5;24(20):3236-45. Erratum in: Oncogene. 2008 Feb 21;27(9):1344. PubMed PMID: 15735720. 15: Joo MK, Park JJ, Kim SH, Yoo HS, Lee BJ, Chun HJ, Lee SW, Bak YT. Antitumorigenic effect of plumbagin by induction of SH2-containing protein tyrosine phosphatase 1 in human gastric cancer cells. Int J Oncol. 2015;46(6):2380-8. doi: 10.3892/ijo.2015.2935. PubMed PMID: 25815436. 16: Chang CW, Tsai WH, Chuang WJ, Lin YS, Wu JJ, Liu CC, Tsai PJ, Lin MT. Procaspase 8 and Bax are up-regulated by distinct pathways in Streptococcal pyrogenic exotoxin B-induced apoptosis. J Biol Chem. 2009 Nov 27;284(48):33195-205. doi: 10.1074/jbc.M109.020586. PubMed PMID: 19801665; PubMed Central PMCID: PMC2785162. 17: Miike S, Nakao A, Hiraguri M, Kurasawa K, Saito Y, Iwamoto I. Involvement of JAK2, but not PI 3-kinase/Akt and MAP kinase pathways, in anti-apoptotic signals of GM-CSF in human eosinophils. J Leukoc Biol. 1999 May;65(5):700-6. PubMed PMID: 10331501. 18: Marchetti M, Castoldi E, Spronk HM, van Oerle R, Balducci D, Barbui T, Rosing J, Ten Cate H, Falanga A. Thrombin generation and activated protein C resistance in patients with essential thrombocythemia and polycythemia vera. Blood. 2008 Nov 15;112(10):4061-8. doi: 10.1182/blood-2008-06-164087. PubMed PMID: 18768782. 19: Peng HX, Wu WQ, Yang DM, Jing R, Li J, Zhou FL, Jin YF, Wang SY, Chu YM. Role of B7-H4 siRNA in Proliferation, Migration, and Invasion of LOVO Colorectal Carcinoma Cell Line. Biomed Res Int. 2015;2015:326981. doi: 10.1155/2015/326981. PubMed PMID: 26078947; PubMed Central PMCID: PMC4454715. 20: An HJ, Choi EK, Kim JS, Hong SW, Moon JH, Shin JS, Ha SH, Kim KP, Hong YS, Lee JL, Choi EK, Lee JS, Jin DH, Kim TW. INCB018424 induces apoptotic cell death through the suppression of pJAK1 in human colon cancer cells. Neoplasma. 2014;61(1):56-62. PubMed PMID: 24195509.