PNU-159682
PNU-159682
CAS: 202350-68-3
Molecular Formula: C32H35NO13
PNU-159682 - Names and Identifiers
| Name | PNU-159682 |
| Synonyms | PNU159682 PNU-159682 |
| CAS | 202350-68-3 |
PNU-159682 - Physico-chemical Properties
| Molecular Formula | C32H35NO13 |
| Molar Mass | 641.62 |
| Density | 1.58±0.1 g/cm3(Predicted) |
| Boling Point | 838.5±65.0 °C(Predicted) |
| Solubility | 10 mM in DMSO |
| pKa | 7.34±0.60(Predicted) |
| Storage Condition | under inert gas (nitrogen or Argon) at 2–8 °C |
| In vitro study | PNU-159682 (0-500 nM; exposed to the compounds for 1 hour and then cultured in compound-free medium for 72 hours) has cytotoxic effects on human tumor cell lines in a sulforhodamine B assay. The IC 70 values are 0.577 nM, 0.39 nM, 0.128 nM, and 0.081 nM, 0.086 nM and 0.075 nM for HT-29, A2780, DU145, EM-2, Jurkat and CEM cells, respectively. It against human tumor cell lines with IC 70 in the ranging 68 nM-578 nM and 181 nM-1717 nM towards MMDX and doxorubicin, respectively. PNU-159682 is more potent than MMAE on NHL cell lines. In a cell viability assay, PNU-159682 is against BJAB.Luc, Granta-519, SuDHL4.Luc, and WSU-DLCL2 with IC 50 values of 0.10 nM, 0.020 nM, 0.055 nM, and 0.1 nM, respectively. While MMAE is against BJAB.Luc, Granta-519, SuDHL4.Luc, and WSU-DLCL2 with IC 50 values of 0.54 nM, 0.25 nM, 1.19 nM and 0.25 nM, respectively.PNU-159682 is thousands of times more cytotoxic than doxorubicin and can be used to develop a new class of ADCs. PNU159682toanti-CD22antibody (anti-CD22-NMS249) exhibits strong anti-tumor effects in vitro . Anti-CD22-NMS249 (PNU159682toanti-CD22antibody) is active in in vitro viability assays of NHL cell lines and is 2 to 20 fold more potent than pinatuzumab vedotin, the ADC anti-CD22-NMS249 is against BJAB.Luc, Granta-519, SuDHL4.Luc, and WSU-DLCL2 with IC 50 values of 0.058 nM, 0.030 nM, 0.0221 nM, and 0.01 nM, respectively.PNU-159682 (100 μM) weakly inhibits topoisomerase II unknotting activity. PNU-159682 shows cytotoxic effect on CAIX-expressing SKRC-52 cells with IC 50 of 25 nM. Cell Viability Assay Cell Line: HT-29, A2780, DU145, EM-2, Jurkat and CEM cells Concentration: 0-500 nM Incubation Time: Exposed to the PNU-159682 for 1 hour and then cultured in compound-free medium for 72 hours Result: Was 2,360- to 790-fold and 6,420- to 2,100-fold more potent than MMDX and doxorubicin, respectively. Exhibited IC 70 values of PNU-159682 are in the subnanomolar range (0.07-0.58 nM) and noticeably lower than that recorded for both MMDX and doxorubicin. |
| In vivo study | PNU-159682 (single-dose; i.v.15 μg/kg) is a maximum tolerated dose in murine L1210 leukemia model. PNU-159682 shows an improved antitumor activity in vivo. The antitumor effect of PNU-159682 (increase in life span=29%) is comparable to that afforded by 90 μg/kg MMDX (increase in life=36%).PNU-159682 (i.v. 4 μg/kg; q7dx3; 40 days) has a therapeutic response in MX-1 human mammary carcinoma mice. What’s more, from day 39, four out of seven mice receiving PNU-159682 exhibits complete tumor regression.PNU-159682 is more cytotoxic than doxorubicin and can be used to develop a new class of ADCs. PNU159682toanti-CD22antibody (anti-CD22-NMS249) exhibits strong anti-tumor effects in vivo . ADC dose (anti-CD22-NMS249; 50 µg/m2 conjugated PNU-159682) is well tolerated in mice and results in less than 10% weight loss.In the BJAB.Luc model the efficacy of antiCD22-NMS249 (single dose; 2 mg/kg) is similar to anti-CD22-vc-MMAE. At 2 mg/kg dosage, antiCD22-NMS249 gives complete remission of the tumors (NMS249: 110-134%TGI vs. vc-MMAE: 114-143%TGI). Additionally, a single dose of antiCD22-NMS249 at 2 mg/kg results in tumor stasis for three weeks. Animal Model: Four- to six-week-old female CD-1 athymic nude mice with MX-1 tumor fragments Dosage: 4 μg/kg Administration: Intravenous injection; q7dx3; 40 days Result: Exhibited anti-cancer effects in MX-1 human mammary carcinoma xenografts to PNU-159682. |
PNU-159682 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.559 ml | 7.793 ml | 15.586 ml |
| 5 mM | 0.312 ml | 1.559 ml | 3.117 ml |
| 10 mM | 0.156 ml | 0.779 ml | 1.559 ml |
| 5 mM | 0.031 ml | 0.156 ml | 0.312 ml |
Last Update：2024-01-02 23:10:35
PNU-159682 - Introduction
PNU-159682 is a chemical substance that has the following properties:
1. Appearance: PNU-159682 is a solid substance, which may appear as powder or crystal form.
2. Chemical structure: the specific chemical structure of the PNU-159682 is unknown because there is no detailed information.
3. Dissociation constant: The dissociation constant of the PNU-159682 is also unknown.
The purpose and scope of application of the PNU-159682 is unknown, and there is no public literature and information to provide detailed instructions for its use.
As for the preparation method of PNU-159682:
Due to the lack of detailed information and literature citations, the preparation method and synthesis path of the PNU-159682 are not clear.
When handling and using PNU-159682, pay attention to the following safety information:
1. Toxicity: As detailed information is not available, the toxicity and danger of the PNU-159682 cannot be determined.
2. Contact and inhalation: any chemical substances should avoid direct skin contact and inhalation. So for PNU-159682, also need to pay attention to avoid contact and inhalation.
3. Environment: The treatment and disposal of chemicals should meet the requirements of environmental protection.
4. Follow laboratory safety practices: Always follow laboratory safety practices and use appropriate personal protective equipment (such as lab gloves, protective glasses, and laboratory ventilation) when handling any chemical.
1. Appearance: PNU-159682 is a solid substance, which may appear as powder or crystal form.
2. Chemical structure: the specific chemical structure of the PNU-159682 is unknown because there is no detailed information.
3. Dissociation constant: The dissociation constant of the PNU-159682 is also unknown.
The purpose and scope of application of the PNU-159682 is unknown, and there is no public literature and information to provide detailed instructions for its use.
As for the preparation method of PNU-159682:
Due to the lack of detailed information and literature citations, the preparation method and synthesis path of the PNU-159682 are not clear.
When handling and using PNU-159682, pay attention to the following safety information:
1. Toxicity: As detailed information is not available, the toxicity and danger of the PNU-159682 cannot be determined.
2. Contact and inhalation: any chemical substances should avoid direct skin contact and inhalation. So for PNU-159682, also need to pay attention to avoid contact and inhalation.
3. Environment: The treatment and disposal of chemicals should meet the requirements of environmental protection.
4. Follow laboratory safety practices: Always follow laboratory safety practices and use appropriate personal protective equipment (such as lab gloves, protective glasses, and laboratory ventilation) when handling any chemical.
Last Update：2024-04-09 22:09:11
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View History
PNU-159682
10265-70-0
34041-09-3
trans-4-Undecensaeure
Iloperidone
Difurfurylsulfide
ALIZARIN BLUE GS
H-D-THR-OBZL HCL
Pomalidomide-C2-NH2 hydrochloride
Pimelic acid dimethyl
10265-70-0
34041-09-3
trans-4-Undecensaeure
Iloperidone
Difurfurylsulfide
ALIZARIN BLUE GS
H-D-THR-OBZL HCL
Pomalidomide-C2-NH2 hydrochloride
Pimelic acid dimethyl