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Purity: ≥98%
CUDC-427 (also known as GDC-0917) is a novel, potent, orally available, second-generation antagonist of inhibitor of apoptosis (IAP) proteins that is being developed for the treatment of various cancers. In the mouse (12.0 ml/min/kg), rat (27.0 ml/min/kg), and dog (15.3 ml/min/kg), GDC-0917 is cleared in a low to moderate amount, whereas the clearance in the monkey (67.6 ml/min/kg) is high. As a result, when compared to other species, monkeys had the lowest oral bioavailability. In vitro-in vivo extrapolation was used to forecast a moderate clearance (11.5 ml/min/kg) in people based on our experience with a prototype molecule with a comparable structure. Simple allometry was used to calculate a 6.69 l/kg estimate for the predicted human volume of distribution.
| ln Vitro |
GDC-0917 (0.1 nM-10 μM) icauses a concentration-dependent decrease in cIAP1 levels in PBMCs, with greater than 80% inhibition at concentrations higher than 0.1 µM (56.5 ng/mL)[1].
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| ln Vivo |
GDC-0917 is well tolerated, with all dose groups experiencing a <11% decrease in mean body weight. GDC-0917 (0.08-16.3 mg/kg) exhibits antitumor activity in a dose dependent manner in the MDA-MB-231-X1.1 Breast Cancer Xenograft. In the mouse (12.0 mL/min/kg), rat (27.0 mL/min/kg), and dog (15.3 mL/min/kg), GDC-0917 is cleared in a low to moderate amount, whereas the clearance in the monkey (67.6 mL/min/kg) is high. Monkeys have the lowest oral bioavailability of any species[1].
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| References |
| Molecular Formula |
C29H36N6O4S
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|---|---|
| Molecular Weight |
564.698945045471
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| Exact Mass |
564.25
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| Elemental Analysis |
C, 61.68; H, 6.43; N, 14.88; O, 11.33; S, 5.68
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| CAS # |
1446182-94-0
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| Related CAS # |
1446182-94-0
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| Appearance |
white solid powder
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| SMILES |
C[C@@H](C(=O)N[C@@H](C1CCCCC1)C(=O)N2CCC[C@H]2C(=O)NC3=C(N=C(S3)C4=NC=CO4)C5=CC=CC=C5)NC
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| InChi Key |
HSHPBORBOJIXSQ-HARLFGEKSA-N
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| InChi Code |
InChI=1S/C29H36N6O4S/c1-18(30-2)24(36)32-23(20-12-7-4-8-13-20)29(38)35-16-9-14-21(35)25(37)34-27-22(19-10-5-3-6-11-19)33-28(40-27)26-31-15-17-39-26/h3,5-6,10-11,15,17-18,20-21,23,30H,4,7-9,12-14,16H2,1-2H3,(H,32,36)(H,34,37)/t18-,21-,23-/m0/s1
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| Chemical Name |
(2S)-1-[(2S)-2-cyclohexyl-2-[[(2S)-2-(methylamino)propanoyl]amino]acetyl]-N-[2-(1,3-oxazol-2-yl)-4-phenyl-1,3-thiazol-5-yl]pyrrolidine-2-carboxamide
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| Synonyms |
CUDC427; CUDC-427; CUDC 427; GDC0917; GDC-0917; GDC 0917
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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: ~50 mg/mL (~88.54 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.43 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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 25.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7709 mL | 8.8543 mL | 17.7085 mL | |
| 5 mM | 0.3542 mL | 1.7709 mL | 3.5417 mL | |
| 10 mM | 0.1771 mL | 0.8854 mL | 1.7709 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 |
| NCT01226277 | Completed | Drug: GDC-0917 | Solid Cancers | Genentech, Inc. | October 2010 | Phase 1 |
| NCT01908413 | Terminated | Drug: CUDC-427 | Lymphoma | Curis, Inc. | July 2013 | Phase 1 |
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