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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
48 Results for "
tolerability
" in MedChemExpress (MCE) Product Catalog:
Products (48)
48 Results for "tolerability" in MCE Product Catalog:
17
17 Publications Verification
RMC-7977 is an orally active triple-complex RAS inhibitor that can simultaneously bind to cyclophilin A (CYPA) (Kd = 195 nM) and KRAS (G12V) (Kd = 292 μM). It exhibits broad-spectrum inhibitory activity against KRAS, NRAS, and HRAS proteins and their various wild-type and mutant variants. RMC-7977 induces apoptosis by inhibiting the phosphorylation of ERK, CRAF, and RSK, as well as increasing PARP cleavage. This leads to tumor regression, reduces resistance in KRAS G12C cancer models, and demonstrates good tolerability across various RAS cancer models .
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11 Cited Publications
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ABBV-744 is a first-in-class, orally active and selective inhibitor of the BDII domain of BET family proteins with IC50 values ranging from 4 to 18 nM for BRD2, BRD3, BRD4 and BRDT. ABBV-744 is primarily metabolized by CYP3A4 with agent-like properties enable the investigation of its antitumor efficacy and tolerability .
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7 Cited Publications
Cat. No.: HY-P99974
Synonyms: Nanoparticle albumin-bound Paclitaxel; Nanoparticle albumin-bound ABI-007
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MS-444 (BE-34776) is a HuR (ELAVL1) inhibitor that blocks the cytoplasmic translocation of HuR and inhibits its dimerization. MS-444 reduces cytoplasmic HuR levels by preventing the binding of HuR to ARE-mRNA, without altering the total expression of HuR. MS-444 induces apoptosis, inhibits cell growth, angiogenesis and invasion, and also regulates immune function and microbiota. MS-444 effectively alters the number, size and invasiveness of tumors in various cancer models. MS-444 is tolerable to intraperitoneal injection in vivo and can be applied to research related to colorectal cancer, familial adenomatous polyposis, colitis-associated cancer and glioblastoma .
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3 Cited Publications
Cat. No.: HY-17552
CAS No.: 28319-77-9
Synonyms: Choline Alfoscerate; Alpha-GPC; L-α-GPC
1
Sitneprotafib (JAB-3312) is an orally effective anticancer phosphatase SHP2 inhibitor (IC50: 1.9 nM) with anti-cancer activity. Sitneprotafib has good tolerability and significantly induced tumor regression in a KYSE-520 mouse xenograft model .
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ALZ-801 is a potent and orally available small-molecule β-amyloid (Aβ) anti-oligomer and aggregation inhibitor, valine-conjugated proagent of Tramiprosate with substantially improved PK properties and gastrointestinal tolerability compared with the parent compound . ALZ-801 is an advanced and markedly improved candidate for the treatment of alzheimer’s disease .
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Dornase alfa (rhDNase) is a recombinant human deoxyribonuclease I (rhDNase) that can specifically degrade extracellular DNA. Dornase alfa catalyzes the cleavage of DNA released by neutrophils in respiratory mucus, reduces sputum viscosity, thereby improving mucus clearance efficiency, reducing airway obstruction and alleviating inflammatory responses. Dornase alfa can be used to improve lung function (such as FEV_1) in cystic fibrosis (CF), reduce the risk of acute pulmonary exacerbations, and has good in vivo tolerability. Dornase alfa acts locally on the respiratory tract through aerosol inhalation, specifically improving the high viscosity of mucus caused by DNA accumulation and related respiratory symptoms .
Cat. No.: HY-P3375
CAS No.: 2259884-03-0
Synonyms: IBI-362; LY-3305677; OXM-3
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Cat. No.: HY-P99116
CAS No.: 1607793-29-2
Synonyms: RG7716; RO-6867461
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Cat. No.: HY-P990774
CAS No.: 2768386-15-6
Synonyms: ASP-7266; TRAB-1; UPB-101
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Cat. No.: HY-175199
CAS No.: 2404652-24-8
Synonyms: BPN-0026709
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MT-228 (BPN-0026709) is a selective and blood-brain barrier permeable non-muscle myosin II inhibitor. MT-228 markedly improves tolerability by selectively targeting NMIIB (KI = 1.5 μM) over CMII (KI = 17 μM), and the sequence of SmMll MD is 83.6% identical to that of NMllB. MT-228 shows long-lasting efficacy in animal models of stimulant use disorder .
Cat. No.: HY-P3375A
Synonyms: IBI-362 TFA; LY-3305677 TFA; OXM-3 TFA
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Cat. No.: HY-159821
CAS No.: 2830607-59-3
Synonyms: CK-4021586; CK-586
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Ulacamten (CK-4021586; CK-586) is an orally active cardiac myosin inhibitor and an inhibitor of the double-headed cardiac heavy meromyosin (HMM)ATPase (excluding single-headed myosin subfragment-1), with an EC50 of 2.9 μM. Ulacamten regulates cardiac myosin, reduces excessive myocardial contractility, and alleviates left ventricular outflow tract obstruction. Ulacamten increases the left ventricular short-axis systolic internal diameter, inhibits dobutamine-induced exacerbation of obstruction, and exerts only a mild reducing effect on left ventricular systolic function. Ulacamten also inhibits the fractional shortening of the short axis without altering calcium transients. Ulacamten shows good safety and tolerability in purpose-bred cats with naturally occurring obstructive hypertrophic cardiomyopathy .
Senexin C is a selective and orally active CDK8/19 inhibitor. Senexin C shows a strong tumor-enrichment pharmacokinetic (PK) profile and tumor-pharmacodynamic (PD) marker responses. Senexin C inhibits the growth of MV4-11 leukemia cells with good tolerability .
Cat. No.: HY-175668
CAS No.: 2756581-81-2
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IDOR-1104-0086 is an orally active Kv7 potassium channel opener with an EC50 of 210 nM that can cross blood-brain barrier. IDOR-1104-0086 displays strong selectivity against the hERG channel with an IC20 of 25 μM. IDOR-1104-0086 exhibits efficacy in two rodent models of epilepsy and a favorable tolerability profile. IDOR-1104-0086 can used for the study of epilepsy .
Synonyms: TC-1734; ACD3480
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Ispronicline (TC-1734), an orally active, brain-selective α4β2 nicotine acetylcholine receptor (nAChR) partial agonist, has shown memory-enhancing properties in rodents and a good tolerability profile. Ispronicline binds to the α4β2 nAChR with high affinity (Ki=11 nM) and is highly selective to other nAChRs such as α7 nAChR and α3β4 nAChR .
Cat. No.: HY-17552R
CAS No.: 28319-77-9
Synonyms: Choline Alfoscerate (Standard); Alpha-GPC (Standard); L-α-GPC (Standard)
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Nur77 modulator 1 is a good Nur77 binder (KD = 3.58 μM). Nur77 modulator 1 up-regulates Nur77 expression, mediates sub-cellular localization of Nur77, induces Nur77-dependent ER stress and autophagy, and results in cell apoptosis. Anti-hepatoma activity .
Cat. No.: HY-14913
CAS No.: 160707-69-7
Synonyms: SPD754; AVX754
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Apricitabine (SPD754; AVX754), the (-) enantiomer of 2′-deoxy-3′-oxa-4′-thiocytidine (dOTC), is a highly selective and orally active HIV-1 reverse transcriptase (RT) inhibitor (Ki=0.08 μM), as well as inhibits DNA polymerases α, β, and γ with Ki value of 300 μM, 12 μM, and 112.25 μM, respectively . Apricitabine (SPD754; AVX754) shows promising antiretroviral efficacy, good tolerability and a low propensity for resistance selection in antiretroviral-naive HIV infection .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
