Size | Price | Stock | Qty |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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XL999, a Spectrum Selective Kinase Inhibitor(TM) (SSKIs), is a potent inhibitor of key RTKs implicated in the development and maintenance of tumor vasculature and in the proliferation of some tumor cells. It inhibits the FGFR, VEGFR and PDGFR RTKs and exhibited excellent activity in target-specific cellular functional assays. In addition, XL999 is a potent inhibitor of FLT3, an important driver of leukemia cell proliferation in some patients with acute myelogenous leukemia (AML). In several preclinical models of human tumors, including breast, lung, colon and prostate cancer, XL999 demonstrated potent inhibition of tumor growth, and also caused regression of large well-established tumors.
Targets |
Flt-1 (IC50 = 4 nM); KDR (IC50 = 20 nM); PDGFRα (IC50 = 4 nM); FGFR1 (IC50 = 2 nM)
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ln Vitro |
The source of tyrosine kinase-IN-1 was compound 8K [1].
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ln Vivo |
The PK profile of tyrosine kinase-IN-1 was reasonable (AUC(0–∞)=1.9, t1/2=4.6 h). In rats, it has a high oral bioavailability (F=63%) [1].
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References |
[1]. Moon K, et al. The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors. Bioorganic & Medicinal Chemistry Letters 22 (2012) 4979–4985
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Molecular Formula |
C26H28FN5O
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Molecular Weight |
445.5424
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Exact Mass |
445.23
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Elemental Analysis |
C, 70.09; H, 6.33; F, 4.26; N, 15.72; O, 3.59
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CAS # |
705946-27-6
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Related CAS # |
705946-27-6
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Appearance |
Solid powder
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SMILES |
CCN1CCC(CC1)NC2=CC\3=C(C=C2)NC(=O)/C3=C(/C4=CC(=CC=C4)F)\C5=NC=C(N5)C
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InChi Key |
DMQYDVBIPXAAJA-VHXPQNKSSA-N
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InChi Code |
InChI=1S/C26H28FN5O/c1-3-32-11-9-19(10-12-32)30-20-7-8-22-21(14-20)24(26(33)31-22)23(25-28-15-16(2)29-25)17-5-4-6-18(27)13-17/h4-8,13-15,19,30H,3,9-12H2,1-2H3,(H,28,29)(H,31,33)/b24-23-
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Chemical Name |
(3Z)-5-[(1-ethylpiperidin-4-yl)amino]-3-[(3-fluorophenyl)-(5-methyl-1H-imidazol-2-yl)methylidene]-1H-indol-2-one
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Synonyms |
XL999; XL-999; XL 999
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: ≥ 62.5 mg/mL (~140.3 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.67 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.67 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.2445 mL | 11.2223 mL | 22.4447 mL | |
5 mM | 0.4489 mL | 2.2445 mL | 4.4889 mL | |
10 mM | 0.2244 mL | 1.1222 mL | 2.2445 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT00955084 | Completed | Drug: XL999 | Advanced Malignancies | Symphony Evolution, Inc. | August 2008 | Phase 1 |
NCT00104117 | Completed | Drug: XL999 | Cancer | Symphony Evolution, Inc. | November 2004 | Phase 1 |
NCT00491699 | Terminated | Drug: XL999 | Non-Small-Cell Lung Cancer | Symphony Evolution, Inc. | August 2007 | Phase 1 |
NCT00322673 | Terminated | Drug: XL999 | Acute Myeloid Leukemia AML |
Symphony Evolution, Inc. | May 2006 | Phase 2 |
NCT00277290 | Terminated | Drug: XL999 | Ovarian Cancer | Symphony Evolution, Inc. | January 2006 | Phase 2 |
XL880, XL184, and XL999 effects on tumor vessels. Cancer Res . 2011 Jul 15;71(14):4758-68. td> |