SNX-2112 | PF-04928473 | CAS#908112-43-6 | Hsp90 inhibitor

MedKoo Cat#: 205736 | Name: SNX-2112

Description:

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

SNX-2112, also known as PF 04928473, is an Hsp90 inhibitor which is currently undergoing multiple phase 1 clinical trials. In all cell lines, SNX-2112 led to degradation of MET, HER-2, EGFR, and AKT as well as abrogation of Ras/Raf/MEK/MAPK and PI3K/AKT signaling, followed by complete cell cycle arrest.

Chemical Structure

SNX-2112

CAS#908112-43-6

Theoretical Analysis

MedKoo Cat#: 205736

Name: SNX-2112

CAS#: 908112-43-6

Chemical Formula: C23H27F3N4O3

Exact Mass: 464.2035

Molecular Weight: 464.48

Elemental Analysis: C, 59.47; H, 5.86; F, 12.27; N, 12.06; O, 10.33

Price and Availability

Size	Price	Availability
10mg	USD 110.00	Ready to ship
25mg	USD 225.00	Ready to ship
50mg	USD 385.00	Ready to ship
100mg	USD 685.00	Ready to ship
200mg	USD 1,250.00	Ready to ship
500mg	USD 2,650.00	Ready to ship
1g	USD 4,350.00	Ready to ship
2g	USD 6,450.00	Ready to ship

Bulk Inquiry

Buy Now

Add to Cart

Related CAS #

No Data

Synonym

SNX2112; SNX-2112; SNX 2112; PF 04928473; PF-04928473; PF04928473.

IUPAC/Chemical Name

4-(6,6-dimethyl-4-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-indazol-1-yl)-2-(((1r,4r)-4-hydroxycyclohexyl)amino)benzamide

InChi Key

ZFVRYNYOPQZKDG-MQMHXKEQSA-N

InChi Code

InChI=1S/C23H27F3N4O3/c1-22(2)10-17-19(18(32)11-22)20(23(24,25)26)29-30(17)13-5-8-15(21(27)33)16(9-13)28-12-3-6-14(31)7-4-12/h5,8-9,12,14,28,31H,3-4,6-7,10-11H2,1-2H3,(H2,27,33)/t12-,14-

SMILES Code

O=C(N)C1=CC=C(N2N=C(C(F)(F)F)C3=C2CC(C)(C)CC3=O)C=C1N[C@H]4CC[C@H](O)CC4

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, not in water

Shelf Life

>5 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

Certificate of Analysis

View CoA: current batch, Lot#C8R05C15

View CoA: current batch, Lot#A8T05K29

QC Data

View QC data: current batch, Lot#C8R05C15

View QC data: current batch, Lot#A8T05K29

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

SNX-2112 selectively binds to the ATP pocket of HSP90α and HSP90β with Ka of 30 nM and 30 nM. SNX-2112 inhibits proliferation in a panel of cancer cell lines (IC50s = 10-50 nM).

In vitro activity:

SNX-2112 has potential in the treatment of non-small cell lung cancer (NSCLC). SNX-2112 promoted cell death and hindered the growth, invasion, and movement of NSCLC cells in vitro. This study identified the mechanism involved, revealing that SNX-2112 suppressed epithelial-mesenchymal transition (EMT) and the Wnt/β-catenin signaling pathway in NSCLC cells. Reference: J Cancer. 2021 Aug 3;12(19):5825-5837. https://pubmed.ncbi.nlm.nih.gov/34475996/

In vivo activity:

SNX-2112 has the potential to improve patient outcome in multiple myeloma (MM) and other blood cancers. In a mouse model, SNX-2112, delivered as SNX-5422, slowed MM growth and extended survival. SNX-2112 also prevented the formation of blood vessels and inhibited bone cell development. Reference: Blood. 2009 Jan 22;113(4):846-55. https://pubmed.ncbi.nlm.nih.gov/18948577/

	Solvent	mg/mL	mM
Solubility
	DMSO	47.0	101.19
	DMSO:PBS (pH 7.2) (1:1)	0.5	1.08
	DMF	0.3	0.54
	Ethanol	1.0	2.15

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 464.48 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. Cheng X, Qin L, Deng L, Zhu X, Li Y, Wu X, Zheng Y. SNX-2112 Induces Apoptosis and Inhibits Proliferation, Invasion, and Migration of Non-Small Cell Lung Cancer by Downregulating Epithelial-Mesenchymal Transition via the Wnt/β-Catenin Signaling Pathway. J Cancer. 2021 Aug 3;12(19):5825-5837. doi: 10.7150/jca.56640. PMID: 34475996; PMCID: PMC8408115. 2. Hu L, Wang Y, Chen Z, Fu L, Wang S, Zhang X, Zhang P, Lu X, Jie H, Li M, Wang Y, Liu Z. Hsp90 Inhibitor SNX-2112 Enhances TRAIL-Induced Apoptosis of Human Cervical Cancer Cells via the ROS-Mediated JNK-p53-Autophagy-DR5 Pathway. Oxid Med Cell Longev. 2019 Mar 25;2019:9675450. doi: 10.1155/2019/9675450. PMID: 31019655; PMCID: PMC6452544. 3. Okawa Y, Hideshima T, Steed P, Vallet S, Hall S, Huang K, Rice J, Barabasz A, Foley B, Ikeda H, Raje N, Kiziltepe T, Yasui H, Enatsu S, Anderson KC. SNX-2112, a selective Hsp90 inhibitor, potently inhibits tumor cell growth, angiogenesis, and osteoclastogenesis in multiple myeloma and other hematologic tumors by abrogating signaling via Akt and ERK. Blood. 2009 Jan 22;113(4):846-55. doi: 10.1182/blood-2008-04-151928. Epub 2008 Oct 23. PMID: 18948577; PMCID: PMC2630270. 4. Chandarlapaty S, Sawai A, Ye Q, Scott A, Silinski M, Huang K, Fadden P, Partdrige J, Hall S, Steed P, Norton L, Rosen N, Solit DB. SNX2112, a synthetic heat shock protein 90 inhibitor, has potent antitumor activity against HER kinase-dependent cancers. Clin Cancer Res. 2008 Jan 1;14(1):240-8. doi: 10.1158/1078-0432.CCR-07-1667. PMID: 18172276; PMCID: PMC3203688.

In vitro protocol:

In vivo protocol:

1. Okawa Y, Hideshima T, Steed P, Vallet S, Hall S, Huang K, Rice J, Barabasz A, Foley B, Ikeda H, Raje N, Kiziltepe T, Yasui H, Enatsu S, Anderson KC. SNX-2112, a selective Hsp90 inhibitor, potently inhibits tumor cell growth, angiogenesis, and osteoclastogenesis in multiple myeloma and other hematologic tumors by abrogating signaling via Akt and ERK. Blood. 2009 Jan 22;113(4):846-55. doi: 10.1182/blood-2008-04-151928. Epub 2008 Oct 23. PMID: 18948577; PMCID: PMC2630270. 2. Chandarlapaty S, Sawai A, Ye Q, Scott A, Silinski M, Huang K, Fadden P, Partdrige J, Hall S, Steed P, Norton L, Rosen N, Solit DB. SNX2112, a synthetic heat shock protein 90 inhibitor, has potent antitumor activity against HER kinase-dependent cancers. Clin Cancer Res. 2008 Jan 1;14(1):240-8. doi: 10.1158/1078-0432.CCR-07-1667. PMID: 18172276; PMCID: PMC3203688.

1: Liu KS, Liu H, Qi JH, Liu QY, Liu Z, Xia M, Xing GW, Wang SX, Wang YF. SNX-2112, an Hsp90 inhibitor, induces apoptosis and autophagy via degradation of Hsp90 client proteins in human melanoma A-375 cells. Cancer Lett. 2011 Dec 17. [Epub ahead of print] PubMed PMID: 22182451. 2: Wang SX, Ju HQ, Liu KS, Zhang JX, Wang X, Xiang YF, Wang R, Liu JY, Liu QY, Xia M, Xing GW, Liu Z, Wang YF. SNX-2112, a novel Hsp90 inhibitor, induces G2/M cell cycle arrest and apoptosis in MCF-7 cells. Biosci Biotechnol Biochem. 2011;75(8):1540-5. Epub 2011 Aug 7. PubMed PMID: 21821931. 3: Chinn DC, Holland WS, Yoon JM, Zwerdling T, Mack PC. Anti-tumor activity of the HSP90 inhibitor SNX-2112 in pediatric cancer cell lines. Pediatr Blood Cancer. 2011 Jul 27. doi: 10.1002/pbc.23270. [Epub ahead of print] PubMed PMID: 21796766. 4: Zhai QQ, Gong GQ, Liu Z, Luo Y, Xia M, Xing GW, You XF, Wang YF. Preclinical pharmacokinetic analysis of SNX-2112, a novel Hsp90 inhibitor, in rats. Biomed Pharmacother. 2011 Mar;65(2):132-6. Epub 2010 Dec 30. PubMed PMID: 21227627. 5: Bachleitner-Hofmann T, Sun MY, Chen CT, Liska D, Zeng Z, Viale A, Olshen AB, Mittlboeck M, Christensen JG, Rosen N, Solit DB, Weiser MR. Antitumor activity of SNX-2112, a synthetic heat shock protein-90 inhibitor, in MET-amplified tumor cells with or without resistance to selective MET Inhibition. Clin Cancer Res. 2011 Jan 1;17(1):122-33. PubMed PMID: 21208906; PubMed Central PMCID: PMC3263825. 6: Zhai QQ, Gong GQ, Luo Y, Wang QD, Xia M, Xing GW, Li YC, Jiang JH, Liu Z, Liu QY, Wang YF. Determination of SNX-2112, a selective Hsp90 inhibitor, in plasma samples by high-performance liquid chromatography and its application to pharmacokinetics in rats. J Pharm Biomed Anal. 2010 Dec 1;53(4):1048-52. Epub 2010 Jul 6. PubMed PMID: 20675090. 7: Jin L, Xiao CL, Lu CH, Xia M, Xing GW, Xiong S, Liu QY, Liu H, Li YC, Ge F, Wang QD, He QY, Wang YF. Transcriptomic and proteomic approach to studying SNX-2112-induced K562 cells apoptosis and anti-leukemia activity in K562-NOD/SCID mice. FEBS Lett. 2009 Jun 18;583(12):1859-66. Epub 2009 May 8. PubMed PMID: 19427857. 8: Rice JW, Veal JM, Barabasz A, Foley B, Fadden P, Scott A, Huang K, Steed P, Hall S. Targeting of multiple signaling pathways by the Hsp90 inhibitor SNX-2112 in EGFR resistance models as a single agent or in combination with erlotinib. Oncol Res. 2009;18(5-6):229-42. PubMed PMID: 20225761. 9: Okawa Y, Hideshima T, Steed P, Vallet S, Hall S, Huang K, Rice J, Barabasz A, Foley B, Ikeda H, Raje N, Kiziltepe T, Yasui H, Enatsu S, Anderson KC. SNX-2112, a selective Hsp90 inhibitor, potently inhibits tumor cell growth, angiogenesis, and osteoclastogenesis in multiple myeloma and other hematologic tumors by abrogating signaling via Akt and ERK. Blood. 2009 Jan 22;113(4):846-55. Epub 2008 Oct 23. PubMed PMID: 18948577; PubMed Central PMCID: PMC2630270.