MA203 |
Catalog No.GC80887
One-Click Copy Product Info
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MA203 is a selective CHK1 PROTAC degrader.
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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In Vivo, MA203 (12 μM; administered in growth medium; 48 h) hydrochloride exerts anti-leukemic effects with no obvious toxicity in a zebrafish larva model xenografted with fluorescently labeled MOLT-4 cells[1].
In Vitro, MA203 (2 μM; 3-24 h) hydrochloride, in combination with HU, significantly reduces CHK1 protein levels and upregulates γH2AX phosphorylation levels in MIA PaCa-2, MOLT-4, and HCT116 cells in a time- and concentration-dependent manner[1]. MA203 (2 μM; 24 h) hydrochloride, with or without HU treatment, degrades CHK1 in MOLM-13 and RS4-11 cells[1]. MA203 (0.5-10 μM; 24 h) hydrochloride, in combination with HU treatment, dose-dependently upregulates γH2AX phosphorylation and p-ATM (S1981) levels, significantly increases γH2AX foci, and exacerbates DNA single-strand breaks in MIA PaCa-2 and MOLT-4 cells[1]. MA203 (2 μM; 24 h) hydrochloride, in combination with 1 mM HU treatment, upregulates γH2AX phosphorylation levels in MOLT-4 and HCT116 cells[1]. MA203 (1-5 μM; 24 h) hydrochloride, in combination with Ara-C treatment, synergistically enhances Ara-C cytotoxicity in MOLT-4 cells, does not affect cell viability and activation status in activated T and B cells, and does not significantly impair cell survival in mouse hematopoietic stem cells (HSCs)[1]. MA203 (2 μM; 7 days) hydrochloride inhibits cell proliferation in MOLT-4 cells but exerts no effect on RPE1 cells[1]. MA203 (1-10 μM; 48 h) hydrochloride, in combination with HU treatment, induces apoptosis in MIA PaCa-2, HCT116, MOLT-4, and MOLM-13 cells, but does not affect cell viability in RPE1, HS-5, and PBMCs[1]. MA203 (2 μM; 16-48 h) hydrochloride, in combination with 1 mM HU treatment, downregulates the protein expression of TCF1/7, CDCA7, RRM2, ORC1, WRN, and claspin, reduces p-CHK1 (S296) levels, promotes G1 phase arrest, increases the proportion of sub-G1 cells, upregulates BAX, BIM, and NOXA while downregulating BCL-XL and XIAP, significantly increases the loss of mitochondrial membrane potential, and enhances the cleavage of caspase-8, caspase-3, and PARP1 in MIA PaCa-2 cells[1]. MA203 hydrochloride potently binds to purified human CHK1 protein, with a binding rate of 97% at 1.0 μM[1].
References:
[1]. Ashry R, et al. Identification of a Proteolysis-Targeting-Chimera that Addresses Activated Checkpoint Kinase-1 Reveals its Non-Catalytic Functions in Tumor Cells. Angewandte Chemie (International ed. in English). 2025 Dec 01;64(49):e202514788.
| Cas No. | SDF | ||
| Formula | C38H45N9O8 | M.Wt | 755.82 |
| Solubility | Storage | Store at -20°C | |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.3231 mL | 6.6153 mL | 13.2307 mL |
| 5 mM | 264.6 μL | 1.3231 mL | 2.6461 mL |
| 10 mM | 132.3 μL | 661.5 μL | 1.3231 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)