| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
GDC-0575 (also called ARRY-575, RG7741) is a novel, potent and selective inhibitor of CHK1 (Check point kinases) which specifically binds to and inhibits CHK1 with an IC50 of 1.2 nM. This enables tumor cells to escape the cell cycle arrest in the S and G2/M phases that is dependent on CHK1, allowing the cells to undergo DNA repair before going through mitosis. In response to DNA damage, the ATP-dependent serine-threonine kinase CHK1 phosphorylates the cdc25 phosphatases. As a result, CHK1 inhibition may make tumor cells more vulnerable to the damaging effects of some chemotherapy drugs on DNA.
| Targets |
Chk1 (IC50 = 1.2 nM)
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
GDC-0575, also known as ARRY-575 or RG7741, is a novel, strong, and selective inhibitor of CHK1 that binds to it specifically and inhibits it with an IC50 of 1.2 nM.
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| Cell Assay |
AML cell lines are plated in triplicate in 96-well plates at a density of 1×104 cells/well, and are then exposed to various treatment scenarios. The XTT Cell Proliferation Kit II is used to measure cell proliferation following a 24-hour incubation period with GDC-0575[3].
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| Animal Protocol |
Mice: Woman in the nude The hind flank of BALB/c mice receives a subcutaneous injection of 2-3×106 melanoma cells in Matrigel. Mice with tumors up to 100 mm3 are given GDC-0575 (25 mg/kg, 50 mg/kg) or vehicle (0.5% w/v methylcellulose and 0.2% v/v Tween 80) orally. Treatment is given for three cycles, one of which consists of three treatment days in a row followed by four days off. Using calipers, the size of the tumor is measured three times a week. Animals are killed when the treatment is stopped for up to six weeks or when the tumor is larger than one centimeter in diameter [1]..
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| References |
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| Molecular Formula |
C16H20BRN5O
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| Molecular Weight |
378.2669
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| Exact Mass |
377.09
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| Elemental Analysis |
C, 50.80; H, 5.33; Br, 21.12; N, 18.51; O, 4.23
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| CAS # |
1196541-47-5
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| Related CAS # |
GDC-0575 dihydrochloride;1657014-42-0;GDC0575 hydrochloride;1196504-54-7
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| PubChem CID |
46917793
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
1.4
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
23
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| Complexity |
460
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1C[C@H](CN(C1)C2=C3C(=CNC3=NC=C2Br)NC(=O)C4CC4)N
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| InChi Key |
BAZRWWGASYWYGB-SNVBAGLBSA-N
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| InChi Code |
InChI=1S/C16H20BrN5O/c17-11-6-19-15-13(14(11)22-5-1-2-10(18)8-22)12(7-20-15)21-16(23)9-3-4-9/h6-7,9-10H,1-5,8,18H2,(H,19,20)(H,21,23)/t10-/m1/s1
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| Chemical Name |
N-[4-[(3R)-3-aminopiperidin-1-yl]-5-bromo-1H-pyrrolo[2,3-b]pyridin-3-yl]cyclopropanecarboxamide
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.61 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 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.61 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 25.0 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 | 2.6436 mL | 13.2181 mL | 26.4361 mL | |
| 5 mM | 0.5287 mL | 2.6436 mL | 5.2872 mL | |
| 10 mM | 0.2644 mL | 1.3218 mL | 2.6436 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 |
| NCT01564251 | Completed | Drug: GDC-0575 Drug: Gemcitabine |
Lymphoma, Solid Tumor | Genentech, Inc. | March 23, 2012 | Phase 1 |
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