IN-1130
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 407172

CAS#: 868612-83-3

Description: IN-1130 is a highly selective small molecule ALK5 inhibitor with >100 fold selectivity over p38α and a panel of 26 other serine/threonine and tyrosine kinases. It is a suppressor of fibrogenic process of unilateral ureteral obstruction in rats underscoring the potential clinical benefits in the treatment of renal fibrosis. By inhibiting of TGF-β signaling, IN1130 ameliorated experimental autoimmune encephalomyelitis, lessened tunical fibrosis and corrected penile curvature in rats, inhibited cancer metastasis in MMTV/c-Neu breast cancer mice, and enhanced CTL response in cancer mice.


Chemical Structure

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IN-1130
CAS# 868612-83-3

Theoretical Analysis

MedKoo Cat#: 407172
Name: IN-1130
CAS#: 868612-83-3
Chemical Formula: C25H20N6O
Exact Mass: 420.16986
Molecular Weight: 420.48
Elemental Analysis: C, 71.41; H, 4.79; N, 19.99; O, 3.80

Price and Availability

Size Price Availability Quantity
5.0mg USD 255.0 2 Weeks
25.0mg USD 670.0 2 Weeks
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Synonym: IN-1130; IN1130; IN 1130.

IUPAC/Chemical Name: 3-((5-(6-Methylpyridin-2-yl)-4-(quinoxalin-6-yl)-1H-imidazol-2-yl) methyl)benzamide

InChi Key: RYKSGWSKILPDDY-UHFFFAOYSA-N

InChi Code: InChI=1S/C25H20N6O/c1-15-4-2-7-20(29-15)24-23(17-8-9-19-21(14-17)28-11-10-27-19)30-22(31-24)13-16-5-3-6-18(12-16)25(26)32/h2-12,14H,13H2,1H3,(H2,26,32)(H,30,31)

SMILES Code: O=C(N)C1=CC=CC(CC2=NC(C3=CC=C4N=CC=NC4=C3)=C(C5=NC(C)=CC=C5)N2)=C1

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

Preparing Stock Solutions

The following data is based on the product molecular weight 420.48 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.

Recalculate based on batch purity %
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

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1: Park CY, Min KN, Son JY, Park SY, Nam JS, Kim DK, Sheen YY. An novel inhibitor of TGF-β type I receptor, IN-1130, blocks breast cancer lung metastasis through inhibition of epithelial-mesenchymal transition. Cancer Lett. 2014 Aug 28;351(1):72-80. doi: 10.1016/j.canlet.2014.05.006. Epub 2014 Jun 2. PubMed PMID: 24887560.

2: Sümpelmann R, Kretz FJ, Luntzer R, de Leeuw TG, Mixa V, Gäbler R, Eich C, Hollmann MW, Osthaus WA. Hydroxyethyl starch 130/0.42/6:1 for perioperative plasma volume replacement in 1130 children: results of an European prospective multicenter observational postauthorization safety study (PASS). Paediatr Anaesth. 2012 Apr;22(4):371-8. doi: 10.1111/j.1460-9592.2011.03776.x. Epub 2011 Dec 23. PubMed PMID: 22211931.

3: Ryu JK, Piao S, Shin HY, Choi MJ, Zhang LW, Jin HR, Kim WJ, Han JY, Hong SS, Park SH, Lee SJ, Kim IH, Lee CR, Kim DK, Mamura M, Kim SJ, Suh JK. IN-1130, a novel transforming growth factor-beta type I receptor kinase (activin receptor-like kinase 5) inhibitor, promotes regression of fibrotic plaque and corrects penile curvature in a rat model of Peyronie's disease. J Sex Med. 2009 May;6(5):1284-96. doi: 10.1111/j.1743-6109.2009.01216.x. Epub 2009 Mar 18. PubMed PMID: 19473283.

4: Lee GT, Hong JH, Mueller TJ, Watson JA, Kwak C, Sheen YY, Kim DK, Kim SJ, Kim IY. Effect of IN-1130, a small molecule inhibitor of transforming growth factor-beta type I receptor/activin receptor-like kinase-5, on prostate cancer cells. J Urol. 2008 Dec;180(6):2660-7. doi: 10.1016/j.juro.2008.08.008. Epub 2008 Oct 31. PubMed PMID: 18951571.

5: Kim YW, Kim YK, Kim DK, Sheen YY. Identification of human cytochrome P450 enzymes involved in the metabolism of IN-1130, a novel activin receptor-like kinase-5 (ALK5) inhibitor. Xenobiotica. 2008 May;38(5):451-64. doi: 10.1080/00498250701871121 . PubMed PMID: 18421620.

6: Moon JA, Kim HT, Cho IS, Sheen YY, Kim DK. IN-1130, a novel transforming growth factor-beta type I receptor kinase (ALK5) inhibitor, suppresses renal fibrosis in obstructive nephropathy. Kidney Int. 2006 Oct;70(7):1234-43. Epub 2006 Aug 23. PubMed PMID: 16929250.

7: PENNINGTON VM. A comparative study of six ataraxics in 1130 neuro-psychiatric cases. Miss Doct. 1956 May;33(12):336-9. PubMed PMID: 13309155.

IN-1130

5.0mg / USD 255.0