NSC-33994 | CAS#82058-16-0 | JAK2 inhibitor

MedKoo Cat#: 562336 | Name: NSC-33994

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Description:

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

NSC-33994 is a selective inhibitor of JAK2.

Chemical Structure

NSC-33994

CAS#82058-16-0

Theoretical Analysis

MedKoo Cat#: 562336

Name: NSC-33994

CAS#: 82058-16-0

Chemical Formula: C28H42N2O2

Exact Mass: 438.3246

Molecular Weight: 438.66

Elemental Analysis: C, 76.67; H, 9.65; N, 6.39; O, 7.29

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 250.00
25mg	USD 640.00

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Related CAS #

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Synonym

NSC-33994; NSC 33994; NSC33994;

IUPAC/Chemical Name

(E)-4,4-(1,2-Diethyl-1,2-ethenediyl)bis[2-[(diethylamino)methyl]phenol]

InChi Key

QFNJFVBKASKGEU-OCEACIFDSA-N

InChi Code

InChI=1S/C28H42N2O2/c1-7-25(21-13-15-27(31)23(17-21)19-29(9-3)10-4)26(8-2)22-14-16-28(32)24(18-22)20-30(11-5)12-6/h13-18,31-32H,7-12,19-20H2,1-6H3/b26-25+

SMILES Code

CC/C(C1=CC=C(O)C(CN(CC)CC)=C1)=C(C2=CC=C(O)C(CN(CC)CC)=C2)/CC

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 33994 (G6) is a selective JAK2 inhibitor, with an IC50 of 60 nM.

In vitro activity:

The most potent compound, G6, inhibited HEL cell growth by greater than 99%. This study found that G6 directly inhibited JAK2-Val617Phe kinase activity in a dose-dependent manner with an IC50 of 60 nM (Fig. 1). G6 reduced the levels of phospho-JAK2 in both a dose- and time-dependent manner (Figs. S1 and S2 in Supplementary data). Reference: Bioorg Med Chem Lett. 2009 Jul 1;19(13):3598-601. https://pubmed.ncbi.nlm.nih.gov/19447617/

In vivo activity:

T98G cells were placed in a semi-solid matrix and injected subcutaneously into the flanks of nude mice. After 90 days of growth, mice began receiving daily intraperitoneal injections of either DMSO or 10 mg/kg G6. Overall, the mice that received G6 had significantly smaller tumor volumes when compared to those that received DMSO. This study found that while the anti-apoptotic Bcl-xL and pro-apoptotic Mcl-1 were not significantly different between the two treatment groups, mice that received G6 had significantly higher levels of pro-apoptotic BIM and BAX (Figure 6B). Reference: PLoS One. 2014 Aug 27;9(8):e105568. https://pubmed.ncbi.nlm.nih.gov/25162558/

Preparing Stock Solutions

The following data is based on the product molecular weight 438.66 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:

1. Karayazi Atici Ö, Urbanska A, Gopinathan SG, Boutillon F, Goffin V, Shemanko CS. ATM Is Required for the Prolactin-Induced HSP90-Mediated Increase in Cellular Viability and Clonogenic Growth After DNA Damage. Endocrinology. 2018 Feb 1;159(2):907-930. doi: 10.1210/en.2017-00652. PMID: 29186352. 2. Kiss R, Polgár T, Kirabo A, Sayyah J, Figueroa NC, List AF, Sokol L, Zuckerman KS, Gali M, Bisht KS, Sayeski PP, Keseru GM. Identification of a novel inhibitor of JAK2 tyrosine kinase by structure-based virtual screening. Bioorg Med Chem Lett. 2009 Jul 1;19(13):3598-601. doi: 10.1016/j.bmcl.2009.04.138. Epub 2009 May 5. PMID: 19447617; PMCID: PMC2812898. 3. Baskin R, Park SO, Keserű GM, Bisht KS, Wamsley HL, Sayeski PP. The Jak2 small molecule inhibitor, G6, reduces the tumorigenic potential of T98G glioblastoma cells in vitro and in vivo. PLoS One. 2014 Aug 27;9(8):e105568. doi: 10.1371/journal.pone.0105568. PMID: 25162558; PMCID: PMC4146502. 4. Jin X, Zhao W, Kirabo A, Park SO, Ho WT, Sayeski PP, Zhao ZJ. Elevated levels of mast cells are involved in pruritus associated with polycythemia vera in JAK2V617F transgenic mice. J Immunol. 2014 Jul 15;193(2):477-84. doi: 10.4049/jimmunol.1301946. Epub 2014 Jun 11. PMID: 24920845.

In vitro protocol:

In vivo protocol:

1. Baskin R, Park SO, Keserű GM, Bisht KS, Wamsley HL, Sayeski PP. The Jak2 small molecule inhibitor, G6, reduces the tumorigenic potential of T98G glioblastoma cells in vitro and in vivo. PLoS One. 2014 Aug 27;9(8):e105568. doi: 10.1371/journal.pone.0105568. PMID: 25162558; PMCID: PMC4146502. 2. Jin X, Zhao W, Kirabo A, Park SO, Ho WT, Sayeski PP, Zhao ZJ. Elevated levels of mast cells are involved in pruritus associated with polycythemia vera in JAK2V617F transgenic mice. J Immunol. 2014 Jul 15;193(2):477-84. doi: 10.4049/jimmunol.1301946. Epub 2014 Jun 11. PMID: 24920845.