NSC-12 | CAS#102586-30-1 | extracellular FGF trap

MedKoo Cat#: 407240 | Name: NSC-12

Featured

Description:

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

NSC-12, also known as NSC 172285, is an extracellular FGF trap with significant implications in cancer therapy. NSC12 inhibited the proliferation of different FGF-dependent tumour cell lines, but had no inhibitory effect on FGF-independent tumour cells expressing a constitutively active FGFR1. In vivo, NSC12 was shown to inhibit FGFR phosphorylation, angiogenesis and primary and metastatic tumour growth of FGF-dependent human and mouse cancer cells. Importantly, there was no systemic toxic effect.

Chemical Structure

NSC-12

CAS#102586-30-1

Theoretical Analysis

MedKoo Cat#: 407240

Name: NSC-12

CAS#: 102586-30-1

Chemical Formula: C24H34F6O3

Exact Mass: 484.2412

Molecular Weight: 484.52

Elemental Analysis: C, 59.49; H, 7.07; F, 23.53; O, 9.91

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 260.00
10mg	USD 440.00
25mg	USD 860.00

Bulk Inquiry

Buy Now

Add to Cart

Related CAS #

No Data

Synonym

NSC-12; NSC 12; NSC12; NSC 172285; NSC-172285; NSC172285.

IUPAC/Chemical Name

(R)-4,4,4-trifluoro-1-((3S,8S,9S,10R,13S,14S,17S)-3-hydroxy-10,13-dimethyl-2,3,4,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl)-3-(trifluoromethyl)butane-1,3-diol

InChi Key

OHKBOEWLASAFLW-YHVBFONYSA-N

InChi Code

InChI=1S/C24H34F6O3/c1-20-9-7-14(31)11-13(20)3-4-15-16-5-6-18(21(16,2)10-8-17(15)20)19(32)12-22(33,23(25,26)27)24(28,29)30/h3,14-19,31-33H,4-12H2,1-2H3/t14-,15-,16-,17-,18+,19+,20-,21-/m0/s1

SMILES Code

C[C@@]12[C@@H]([C@H](O)CC(O)(C(F)(F)F)C(F)(F)F)CC[C@@]1([H])[C@]3([H])CC=C4C[C@@H](O)CC[C@]4(C)[C@@]3([H])CC2

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

>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 12 is an extracellular trap of fibroblast growth factor 2 (FGF2) that binds FGF2 and interferes with its interaction with FGFR1.

In vitro activity:

This study aimed to investigate the role of FGF/FGFR system blockade in WM by using a pan-FGF trap molecule (NSC12). Wide-transcriptome profiling confirmed inhibition of FGFR signaling in NSC12-treated WM cells; unveiling a significant inhibition of MYD88 was also confirmed at the protein level. Importantly, the NSC12-dependent silencing of MYD88 was functionally active, as it led to inhibition of MYD88-driven pathways, such as BTK and SYK, as well as the MYD88-downstream target HCK. Reference: Blood. 2021 May 6;137(18):2495-2508. https://pubmed.ncbi.nlm.nih.gov/33197938/

In vivo activity:

Similar to PTX3 overexpression, administration of the PTX3-derived small molecule FGF trap NSC12 results in a significant inhibition of neovessel density and mast cell recruitment in TRAMP-C2 lesions generated by s.c. injection of tumor cells in syngeneic wild-type mice when compared to grafts grown in animals treated with vehicle (DMSO) or the control compound NSC21 (Figures 5 and 6). Reference: Oncotarget. 2017 Aug 1;8(47):82583-82592. https://pubmed.ncbi.nlm.nih.gov/29137286/

	Solvent	mg/mL	mM
Solubility
	DMF	2.0	4.13
	DMSO	5.2	10.73
	Ethanol	41.5	85.65
	Ethanol:PBS (pH 7.2) (1:2)	0.3	0.68

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 484.52 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. Sacco A, Federico C, Giacomini A, Caprio C, Maccarinelli F, Todoerti K, Favasuli V, Anastasia A, Motta M, Russo D, Rossi G, Bozza N, Castelli R, Neri A, Ronca R, Cattaneo C, Tucci A, Mor M, Presta M, Roccaro AM. Halting the FGF/FGFR axis leads to antitumor activity in Waldenström macroglobulinemia by silencing MYD88. Blood. 2021 May 6;137(18):2495-2508. doi: 10.1182/blood.2020008414. PMID: 33197938. 2. Ronca R, Giacomini A, Di Salle E, Coltrini D, Pagano K, Ragona L, Matarazzo S, Rezzola S, Maiolo D, Torrella R, Moroni E, Mazzieri R, Escobar G, Mor M, Colombo G, Presta M. Long-Pentraxin 3 Derivative as a Small-Molecule FGF Trap for Cancer Therapy. Cancer Cell. 2015 Aug 10;28(2):225-39. doi: 10.1016/j.ccell.2015.07.002. PMID: 26267536. 3. Rezzola S, Ronca R, Loda A, Nawaz MI, Tobia C, Paganini G, Maccarinelli F, Giacomini A, Semeraro F, Mor M, Presta M. The Autocrine FGF/FGFR System in both Skin and Uveal Melanoma: FGF Trapping as a Possible Therapeutic Approach. Cancers (Basel). 2019 Sep 4;11(9):1305. doi: 10.3390/cancers11091305. PMID: 31487962; PMCID: PMC6770058. 4. Ronca R, Tamma R, Coltrini D, Ruggieri S, Presta M, Ribatti D. Fibroblast growth factor modulates mast cell recruitment in a murine model of prostate cancer. Oncotarget. 2017 Aug 1;8(47):82583-82592. doi: 10.18632/oncotarget.19773. PMID: 29137286; PMCID: PMC5669912.

In vitro protocol:

In vivo protocol:

1. Rezzola S, Ronca R, Loda A, Nawaz MI, Tobia C, Paganini G, Maccarinelli F, Giacomini A, Semeraro F, Mor M, Presta M. The Autocrine FGF/FGFR System in both Skin and Uveal Melanoma: FGF Trapping as a Possible Therapeutic Approach. Cancers (Basel). 2019 Sep 4;11(9):1305. doi: 10.3390/cancers11091305. PMID: 31487962; PMCID: PMC6770058. 2. Ronca R, Tamma R, Coltrini D, Ruggieri S, Presta M, Ribatti D. Fibroblast growth factor modulates mast cell recruitment in a murine model of prostate cancer. Oncotarget. 2017 Aug 1;8(47):82583-82592. doi: 10.18632/oncotarget.19773. PMID: 29137286; PMCID: PMC5669912.

1: Ronca R, Giacomini A, Di Salle E, Coltrini D, Pagano K, Ragona L, Matarazzo S, Rezzola S, Maiolo D, Torrella R, Moroni E, Mazzieri R, Escobar G, Mor M, Colombo G, Presta M. Long-Pentraxin 3 Derivative as a Small-Molecule FGF Trap for Cancer Therapy. Cancer Cell. 2015 Aug 10;28(2):225-39. doi: 10.1016/j.ccell.2015.07.002. PubMed PMID: 26267536.