BMS 599626 dihydrochloride

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Cat.No. 5022 - BMS 599626 dihydrochloride | C27H27FN8O3.2HCl
Description: Potent, selective EGFR and ErbB2 inhibitor
Chemical Name: (3S)-3-Morpholinylmethyl-[4-[[1-[(3-fluorophenyl)methyl]-1H-indazol-5-yl]amino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]-carbamate dihydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

Biological Activity

Potent and selective EGFR and ErbB2 inhibitor (IC50 values are 22 nM and 32 nM respectively). Also inhibits HER4 (IC50 = 190 nM). Inhibits EGFR and ErbB2 with 100-fold greater potency than MEK and Lck. Antiproliferative agent in vitro and anti-tumorigenic agent in vivo. Orally bioavailable.

Compound Libraries

BMS 599626 dihydrochloride is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 603.48
Formula C27H27FN8O3.2HCl
Storage Store at -20°C
Purity ≥98% (HPLC)
PubChem ID 90488998
InChI Key SKHKFWSXLCGMNF-IKXQUJFKSA-N
Smiles FC1=CC(CN2N=CC3=C2C=CC(NC4=NC=NN5C4=C(C)C(NC(OC[C@@H]6COCCN6)=O)=C5)=C3)=CC=C1.Cl.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 60.35 100
water 3.02 5mM with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 603.48. Batch specific molecular weights may vary from batch to batch due to solvent 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 1.66 mL 8.29 mL 16.57 mL
5 mM 0.33 mL 1.66 mL 3.31 mL
10 mM 0.17 mL 0.83 mL 1.66 mL
50 mM 0.03 mL 0.17 mL 0.33 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Wong et al (2006) Preclinical antitumor activity of BMS-599626, a pan-HER kinase inhibitor that inhibits HER1/HER2 homodimer and heterodimer signaling. Clin.Cancer Res. 12 6186 PMID: 17062696

Gavai et al (2009) Discovery and preclinical evaluation of [4-[[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbamic acid, (3S)-3-morpholinylmethyl ester (BMS-599626), a selective and orally efficaciou J.Med.Chem. 52 6527 PMID: 19821562


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Citations for BMS 599626 dihydrochloride

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