| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| ln Vitro |
GDC-0575 diHClide is an IC50 of 1.2 nM for a selective, oral bioavailable CHK1 inhibitor. By lowering the quantity of Tyr15-phosphorylated CDK2, GDC-0575 (100 nM) prevents AraC-induced CHK1 activation. The viability of AML cells is unaffected by GDC-0575 (100 nM); whereas, binding to AraC dramatically lowers cell viability and triggers apoptosis. Moreover, normal hematopoietic stem and progenitor cells (HSPC) were unaffected by GDC-0575 with AraC [1]. Most of the 20 melanoma cell lines that were evaluated showed cytotoxic action against GDC-0575, while some cell lines that developed into tumor spheres (TS) were comparatively insensitive [2].
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| ln Vivo |
In mice implanted with U937-Luc cells, GDC-0575 (7.5 mg/kg, oral) nearly totally eradicated the leukemia burden and shown greater efficacy than AraC alone. Moreover, GDC-0575 increased AraC's cytotoxicity in vivo in several primary AML models [1]. In D20 and C002 xenografts, GDC-0575 (25, 50 mg/kg, oral) suppresses tumor growth in a dose-dependent manner [2].
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| References |
[1]. Di Tullio A, et al. The combination of CHK1 inhibitor with G-CSF overrides cytarabine resistance in human acute myeloid leukemia. Nat Commun. 2017 Nov 22;8(1):1679.
[2]. Oo ZY, et al. Endogenous Replication Stress Marks Melanomas Sensitive to CHEK1 Inhibitors In Vivo. Clin Cancer Res. 2018 Jun 15;24(12):2901-2912 |
| Molecular Formula |
C17H23BRCL2N4O
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|---|---|
| Molecular Weight |
450.200721025467
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| CAS # |
1657014-42-0
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| Related CAS # |
GDC-0575;1196541-47-5;GDC0575 hydrochloride;1196504-54-7
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| SMILES |
BrC1C=CC2=C(C(=CN2)NC(C2CC2)=O)C=1N1CCC[C@H](C1)N.Cl.Cl
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 : ~65 mg/mL (~144.06 mM)
H2O : ~25 mg/mL (~55.41 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.17 mg/mL (4.81 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 21.7 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: ≥ 2.17 mg/mL (4.81 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 21.7 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. View More
Solubility in Formulation 3: ≥ 2.17 mg/mL (4.81 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10 mg/mL (22.16 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2212 mL | 11.1062 mL | 22.2124 mL | |
| 5 mM | 0.4442 mL | 2.2212 mL | 4.4425 mL | |
| 10 mM | 0.2221 mL | 1.1106 mL | 2.2212 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.
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