6-Quinolinecarboxamide, 1-acetyl-4-[(5-chloro-2-pyrimidinyl)amino]-1,2,3,4-tetrahydro-2-methyl-, (2S,4R)- manufacturers
- I-BET567
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- $133.00 / 1mg
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2024-10-24
- CAS:1887237-54-8
- Min. Order:
- Purity: 98.00%
- Supply Ability: 10g
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| 6-Quinolinecarboxamide, 1-acetyl-4-[(5-chloro-2-pyrimidinyl)amino]-1,2,3,4-tetrahydro-2-methyl-, (2S,4R)- Basic information |
Product Name: | 6-Quinolinecarboxamide, 1-acetyl-4-[(5-chloro-2-pyrimidinyl)amino]-1,2,3,4-tetrahydro-2-methyl-, (2S,4R)- | Synonyms: | 6-Quinolinecarboxamide, 1-acetyl-4-[(5-chloro-2-pyrimidinyl)amino]-1,2,3,4-tetrahydro-2-methyl-, (2S,4R)-;I-BET567;I BET567,I-BET-567,IBET567;(2S,4R)-1-acetyl-4-[(5-chloropyrimidin-2-yl)amino]-2-methyl-1,2,3,4-tetrahydroquinoline-6-carboxamide | CAS: | 1887237-54-8 | MF: | C17H18ClN5O2 | MW: | 359.81 | EINECS: | | Product Categories: | | Mol File: | 1887237-54-8.mol | |
| 6-Quinolinecarboxamide, 1-acetyl-4-[(5-chloro-2-pyrimidinyl)amino]-1,2,3,4-tetrahydro-2-methyl-, (2S,4R)- Chemical Properties |
Boiling point | 631.2±65.0 °C(Predicted) | density | 1.380±0.06 g/cm3(Predicted) | storage temp. | 4°C, protect from light | solubility | DMSO : 100 mg/mL (277.92 mM; Need ultrasonic) | form | Solid | pka | 15.73±0.60(Predicted) | color | White to off-white |
| 6-Quinolinecarboxamide, 1-acetyl-4-[(5-chloro-2-pyrimidinyl)amino]-1,2,3,4-tetrahydro-2-methyl-, (2S,4R)- Usage And Synthesis |
Biological Activity | I-BET567 is a potent and orally active inhibitor of pan-BET candidate with pIC50s of 6.9 and 7.2 for BRD4 BD1 and BD2, respectively. I-BET567 has been demonstrated efficacy in mouse models of oncology and inflammation[1].
I-BET567 (compound 27) (72 hours; 1.5 nM-30 μM) effectively inhibites the proliferation of human NMC cell line 11060 in vitro with a mean gpIC50 6.2 (0.63 μM)[1].
I-BET567 (compound 27) (3, 10, and 30 mg/kg; p.o.; once daily for 20 days) leads to a significant reduction in tumor growth compared with vehicle controls at both 10 and 30 mg/kg[1].Assessment of Pharmacokinetics (PK) profile of I-BET567 following intravenous infusion and oral administration in male wistar han rat and beagle doga[1]. species dose ivb/poc (mg/kg) CLb (mL/min/kg) CLb,u (mL/min/kg) CLrenal (mL/min/kg) Vss (L/kg) Vss,u (L/kg) t1/2 (h) Fpo (%) fub rat1.3/32510972.410.41.699d0.23 dog1.0/38.1206.91.22.91.8980.41a: Values are mean, n=3 unless otherwise stated. b: IV dose 1h infusion in DMSO and (10%, w/v) Kleptose HPB in saline (2%: 98% (v/v)). c: PO dose vehicle: 1%(w/v) methycellulose (400 cps) (aq). d: Mean n = 2. | References | [1]. Humphreys PG, et al. Design, Synthesis, and Characterization of I-BET567, a Pan-Bromodomain and Extra Terminal (BET) Bromodomain Oral Candidate [published online ahead of print, 2022 Jan 7]. |
| 6-Quinolinecarboxamide, 1-acetyl-4-[(5-chloro-2-pyrimidinyl)amino]-1,2,3,4-tetrahydro-2-methyl-, (2S,4R)- Preparation Products And Raw materials |
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