| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
CDK4/D1 26.9 nM (IC50) CDK6/D1 10.4 nM (IC50)
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|---|---|
| ln Vitro |
On MCL cell lines, BSJ-03-204 (0.0001-100 μM; for 3 or 4 days) has strong anti-proliferative effects[1]. A G1 arrest can be potently induced by BSJ-03-204 (1 μM; for 1 day)[1]. In WT cells, BSJ-03-204 (0.1–5 μM) solely degrades CDK4/6; it does not affect IKZF1/3[1].
|
| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: MCL cell lines (Jeko-1, Mino, Granta-519, Rec-1, and Maver-1 cells) Tested Concentrations: 0.0001- 100 μM Incubation Duration: For 3 or 4 days Experimental Results: Had potent anti-proliferative effects on mantle cell lymphoma (MCL) cell lines. Cell Cycle Analysis[1] Cell Types: Granta-519 cells Tested Concentrations: 1 μM Incubation Duration: For 1 day Experimental Results: Potently induced a G1 arrest. Western Blot Analysis[1] Cell Types: Wildtype (WT) or Crbn-/- Jurkat cells Tested Concentrations: 0.1, 0.5, 1, 5 μM Incubation Duration: For 4 hrs (hours) Experimental Results: Only resulted in Degradation of CDK4/6 in WT cells, not IKZF1/3. |
| References |
| Molecular Formula |
C43H48N10O8
|
|---|---|
| Molecular Weight |
832.903429031372
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| Exact Mass |
832.365
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| CAS # |
2349356-09-6
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| Related CAS # |
BSJ-03-204 triTFA
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| PubChem CID |
139593561
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| Appearance |
Light yellow to green yellow solid powder
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| LogP |
2.2
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
14
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
61
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| Complexity |
1750
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C1C(C(C)=O)=C(C)C2=CN=C(NC3=CC=C(C=N3)N3CCN(CCCCNC(COC4=CC=CC5C(N(C(C=54)=O)C4C(NC(CC4)=O)=O)=O)=O)CC3)N=C2N1C1CCCC1
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| InChi Key |
KDMOCOWXLQOXEB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C43H48N10O8/c1-25-30-23-46-43(49-38(30)52(27-8-3-4-9-27)41(59)36(25)26(2)54)47-33-14-12-28(22-45-33)51-20-18-50(19-21-51)17-6-5-16-44-35(56)24-61-32-11-7-10-29-37(32)42(60)53(40(29)58)31-13-15-34(55)48-39(31)57/h7,10-12,14,22-23,27,31H,3-6,8-9,13,15-21,24H2,1-2H3,(H,44,56)(H,48,55,57)(H,45,46,47,49)
|
| Chemical Name |
N-[4-[4-[6-[(6-acetyl-8-cyclopentyl-5-methyl-7-oxopyrido[2,3-d]pyrimidin-2-yl)amino]pyridin-3-yl]piperazin-1-yl]butyl]-2-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]oxyacetamide
|
| 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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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: ~100 mg/mL (~120.1 mM; with ultrasonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.00 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.2006 mL | 6.0031 mL | 12.0062 mL | |
| 5 mM | 0.2401 mL | 1.2006 mL | 2.4012 mL | |
| 10 mM | 0.1201 mL | 0.6003 mL | 1.2006 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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