FIIN-3
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MedKoo CAT#: 406653

CAS#: 1637735-84-2

Description: FIIN-3 is a potent, selective, irreversible and the next-generation covalent FGFR inhibitor. FIIN-3 is the first inhibitor that can potently inhibit the proliferation of cells dependent upon the gatekeeper mutants of FGFR1 or FGFR2, which confer resistance to first-generation clinical FGFR inhibitors such as NVP-BGJ398 and AZD4547. FIIN-3 has the unprecedented ability to inhibit both the EGF receptor (EGFR) and FGFR covalently by targeting two distinct cysteine residues. FIIN-3 bound with FGFR4 V550L and EGFR L858R.

Chemical Structure

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FIIN-3
CAS# 1637735-84-2
Handing Instruction

Theoretical Analysis

MedKoo Cat#: 406653
Name: FIIN-3
CAS#: 1637735-84-2
Chemical Formula: C34H36Cl2N8O4
Exact Mass: 690.22366
Molecular Weight: 691.60684
Elemental Analysis: C, 59.05; H, 5.25; Cl, 10.25; N, 16.20; O, 9.25

Size Price Shipping out time Quantity
50mg USD 1450 2 Weeks
100mg USD 1850 2 Weeks
200mg USD 2250 2 Weeks
500mg USD 2850 2 Weeks
1g USD 3750 2 Weeks
2g USD 4950 2 Weeks
Inquire bulk and customized quantity
Pricing updated 2021-03-04. Prices are subject to change without notice.

FIIN-3, purity > 98%, is in stock. Minimum 50mg order required. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.

Synonym: FIIN3; FIIN 3; FIIN-3.

IUPAC/Chemical Name: N-(4-((3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-(6-((4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)ureido)methyl)phenyl)acrylamide

InChi Key: SFLKJNSBBVSPFE-UHFFFAOYSA-N

InChi Code: InChI=1S/C34H36Cl2N8O4/c1-5-30(45)40-24-8-6-22(7-9-24)20-44(34(46)41-33-31(35)26(47-3)18-27(48-4)32(33)36)29-19-28(37-21-38-29)39-23-10-12-25(13-11-23)43-16-14-42(2)15-17-43/h5-13,18-19,21H,1,14-17,20H2,2-4H3,(H,40,45)(H,41,46)(H,37,38,39)

SMILES Code: O=C(NC1=CC=C(C=C1)CN(C(NC2=C(C(OC)=CC(OC)=C2Cl)Cl)=O)C3=CC(NC4=CC=C(C=C4)N5CCN(CC5)C)=NC=N3)C=C

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

Handling Instructions:
View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 691.60684 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.

Select a batch to recalculate based on the batch molecular weight:
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: Tan L, Wang J, Tanizaki J, Huang Z, Aref AR, Rusan M, Zhu SJ, Zhang Y, Ercan D, Liao RG, Capelletti M, Zhou W, Hur W, Kim N, Sim T, Gaudet S, Barbie DA, Yeh JR, Yun CH, Hammerman PS, Mohammadi M, Jänne PA, Gray NS. Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors. Proc Natl Acad Sci U S A. 2014 Nov 11;111(45):E4869-77. doi: 10.1073/pnas.1403438111. Epub 2014 Oct 27. PubMed PMID: 25349422; PubMed Central PMCID: PMC4234547.

2: Huang Z, Tan L, Wang H, Liu Y, Blais S, Deng J, Neubert TA, Gray NS, Li X, Mohammadi M. DFG-out mode of inhibition by an irreversible type-1 inhibitor capable of overcoming gate-keeper mutations in FGF receptors. ACS Chem Biol. 2015 Jan 16;10(1):299-309. doi: 10.1021/cb500674s. Epub 2014 Oct 27. PubMed PMID: 25317566; PubMed Central PMCID: PMC4301177.

 

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FIIN-3

10mg / Not available


Additional Information