WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H573243
CAS#: 1821329-75-2 (dihydrochloride)
Description: Derazantinib is a multi-kinase inhibitor with pan-FGFR activity which has shown preliminary therapeutic activity against FGFR2 fusion-positive intrahepatic cholangiocarcinoma (iCCA). Derazantinib dihydrochloride is a salt of Derazantinib.
Hodoodo Cat#: H573243
Name: Derazantinib dihydrochloride
CAS#: 1821329-75-2 (dihydrochloride)
Chemical Formula: C29H31Cl2FN4O
Exact Mass: 540.19
Molecular Weight: 541.490
Elemental Analysis: C, 64.33; H, 5.77; Cl, 13.09; F, 3.51; N, 10.35; O, 2.95
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Related CAS #: 1821329-75-2 (dihydrochloride) 1234356-69-4
Synonym: Derazantinib dihydrochloride
IUPAC/Chemical Name: (R)-6-(2-fluorophenyl)-N-(3-(2-((2-methoxyethyl)amino)ethyl)phenyl)-5,6-dihydrobenzo[h]quinazolin-2-amine dihydrochloride
InChi Key: OLDWOVJAXRWCGT-FBHGDYMESA-N
InChi Code: 1S/C29H29FN4O.2ClH/c1-35-16-15-31-14-13-20-7-6-8-22(17-20)33-29-32-19-21-18-26(24-10-4-5-12-27(24)30)23-9-2-3-11-25(23)28(21)34-29;;/h2-12,17,19,26,31H,13-16,18H2,1H3,(H,32,33,34);2*1H/t26-;;/m1../s1
SMILES Code: Cl.Cl.COCCNCCc1cccc(Nc2ncc3C[C@@H](c4ccccc4F)c5ccccc5c3n2)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
Shelf Life: >3 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:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 541.49 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: | |
In vitro protocol: | |
In vivo protocol: |
1: Gourd E. Derazantinib for intrahepatic cholangiocarcinoma. Lancet Oncol. 2018 Nov 22. pii: S1470-2045(18)30891-X. doi: 10.1016/S1470-2045(18)30891-X. [Epub ahead of print] PubMed PMID: 30473470.
2: Mazzaferro V, El-Rayes BF, Droz Dit Busset M, Cotsoglou C, Harris WP, Damjanov N, Masi G, Rimassa L, Personeni N, Braiteh F, Zagonel V, Papadopoulos KP, Hall T, Wang Y, Schwartz B, Kazakin J, Bhoori S, de Braud F, Shaib WL. Derazantinib (ARQ 087) in advanced or inoperable FGFR2 gene fusion-positive intrahepatic cholangiocarcinoma. Br J Cancer. 2018 Nov 13. doi: 10.1038/s41416-018-0334-0. [Epub ahead of print] PubMed PMID: 30420614.